Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors

ABSTRACT

The disclosure relates to a cyclic urea compound of formula I: 
                         
as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

This application is a Divisional of application Ser. No. 10/770,382filed Feb. 2, 2004 now U.S. Pat. No. 7,354,933, which claims the benefitof U.S. Provisional Application Ser. No. 60/468,685 filed May 7, 2003.

FIELD OF THE INVENTION

The present invention relates to a cyclic urea compound, process for itspreparation, pharmaceutical composition comprising it and itspharmaceutical use, as an inhibitor on a protein kinase. Thus, it isuseful for preventing or treating a physiological disorder capable ofbeing modulated by inhibiting the activity of a protein kinase, such asa solid tumor.

BACKGROUND OF THE INVENTION

Protein kinases belong especially to the following group: EGFR, Fak,FLK-1, FGFR1, FGFR2, FGFR3, FGFR4, FGFR5, flt-1, IGF-1R, KDR, PLK,PDGFR, tie2, VEGFR, AKT, and Raf.

Cancer remains a disease for which the existing treatments are clearlyinsufficient. Certain protein kinases, especially including IGF-1R(Insulin Growth Factor 1 Receptor), play an important role in manycancers. The inhibition of such protein kinases is potentially importantin the chemotherapy of cancers, especially for suppressing the growth orsurvival of tumors.

Protein kinases participate in signaling events that control theactivation, growth and differentiation of cells in response either toextracellular mediators or to changes in the environment. In general,these kinases belong to two groups: those that preferentiallyphosphorylate serine and/or threonine residues and those thatpreferentially phosphorylate tyrosine residues [S. K. Hanks and T.Hunter, FASEB. J., 1995, 9, pages 576-596]. The serine/threonine kinasesare, for example, the isoforms of the protein kinases C [A. C. Newton,J. Biol. Chem., 1995, 270, pages 28495-28498] and a group ofcycline-dependent kinases, for instance cdc2 [J. Pines, Trends inBiochemical Sciences, 1995, 18, pages 195-197]. The tyrosine kinasescomprise growth factor receptors, for instance the epidermal growthfactor (EGF) receptor [S. Iwashita and M. Kobayashi, CellularSignalling, 1992, 4, pages 123-132], and cytosol kinases, for instancep56tck, p59fYn and ZAP-70 and the kinases csk [C. Chan et. al., Ann.Rev. Immunol., 1994, 12, pages 555-592].

Abnormally high levels of kinase protein activity have been implicatedin many diseases, resulting from abnormal cellular functions. This mayarise either directly or indirectly from a dysfunction in the mechanismsfor controlling the kinase activity, linked, for example, to a mutation,an overexpression or an inappropriate activation of the enzyme, or anover- or underproduction of cytokines or of growth factors, alsoinvolved in the transduction of the signals upstream or downstream ofthe kinases. In all these cases, a selective inhibition of the action ofthe kinases offers hope of a beneficial effect.

The type 1 receptor for in the insulin-like growth factor (IGF-I-R) is atransmembrane receptor with tyrosine kinase activity which binds firstlyto IGFI, but also to IGFII and to insulin with lower affinity. Thebinding of IGF1 to its receptor results in oligomerization of thereceptor, the activation of tyrosine kinase, intermolecularautophosphorylation and the phosphorylation of cell substrates (mainsubstrates: IRS1 and Shc). The receptor activated by its ligand inducesmitogenic activity in normal cells. However, IGF-I-R plays an importantrole in “abnormal” growth.

Several clinical reports underline the important role of the IGF-I routein the development of human cancers.

IGF-I-R is often found overexpressed in many types of tumors (breast,colon, lung, sarcoma, etc.) and its presence is often associated with amore aggressive phenotype.

High concentrations of circulating IGF1 are strongly correlated with arisk of prostate cancer, lung cancer and breast cancer.

Furthermore, it has been widely documented that IGF-I-R is necessary forestablishing and maintaining the transformed phenotype in vitro as invivo [Baserga R, Exp. Cell. Res., 1999, 253, pages 1-6]. The kinaseactivity of IGF-I-R is essential for the transformation activity ofseveral oncogenes: EGFR, PDGFR, the large T antigen of the SV40 virus,activated Ras, Raf, and v-Src. The expression of IGF-I-R in normalfibroblasts induces a neoplastic phenotype, which may then result in theformation of a tumor in vivo. The expression of IGF-I-R plays animportant role in substrate-independent growth. IGF-I-R has also beenshown to be a protector in chemotherapy-induced and radiation-inducedapoptosis, and cytokine-induced apoptosis. Furthermore, the inhibitionof endogenous IGF-1-R with a negative dominant, the formation of atriple helix or the expression of an antisense sequence brings aboutsuppression of the transforming activity in vitro and reduction of tumorgrowth in animal models.

FAK is a cytoplasmic tyrosine kinase that plays an important role intransducing the signal transmitted by the integrins, a family ofheterodimeric receptors of cellular adhesion. FAK and the integrins arecolocalized in perimembrane structures known as adhesion plaques. It hasbeen shown in many cell types that the activation of FAK and itsphosphorylation on tyrosine residues and in particular itsautophosphorylation on tyrosine 397 were dependent on the binding of theintegrins to their extracellular ligands and thus induced duringcellular adhesion [L. Komberg, et al. J. Biol. Chem. 267(33): 23439-442(1992)]. The autophosphorylation on tyrosine 397 of FAK is a bindingsite for another tyrosine kinase, Src, via its SH2 domain [Schaller etal. Mol. Cell. Biol. 14: 1680-1688 1994; Xing et al. Mol. Cell. Biol. 5:413-421 1994]. Src can then phosphorylate FAK on tyrosine 925, thusrecruiting the adapter protein Grb2 and inducing in certain cellsactivation of the ras and MAP kinase pathway involved in controllingcellular proliferation [Schlaepfer et al. Nature; 372: 786-791 1994;Schlaepfer et al. Prog. Biophy. Mol. Biol. 71: 435-478 1999; Schlaepferand Hunter, J. Biol. Chem. 272: 13189-13195 1997].

The activation of FAK can thus induce the jun NH₂-terminal kinase (JNK)signaling pathway and result in the progression of the cells to the GIphase of the cellular cycle [Oktay et al., J. Cell. Biol. 145: 1461-14691999]. Phosphatidylinositol-3-OH kinase (PI3-kinase) also binds to FAKon tyrosine 397 and this interaction might be necessary for theactivation of PI3-kinase [Chen and Guan, Proc. Nat. Acad. Sci. USA. 91:10148-10152 1994; Ling et al. J. Cell. Biochem. 73: 533-544 1999]. TheFAK/Src complex phosphorylates various substrates, for instance paxillinand p130CAS in fibroblasts [Vuori et al. Mol. Cell. Biol. 16: 2606-26131996].

The results of numerous studies support the hypothesis that FAKinhibitors might be useful in treating cancer. Studies have suggestedthat FAK might play an important role in in vitro cell proliferationand/or survival. For example, in CHO cells, certain authors havedemonstrated that the overexpression of p125FAK induces an accelerationof the G1 to S transition, suggesting that p125FAK promotes cellularproliferation [J. -H. Zhao et al. J. Cell Biol. 143: 1997-2008 1998].Other authors have shown that tumor cells treated with FAK antisenseoligonucleotides lose their adhesion and go into apoptosis (Xu et al,Cell Growth Differ. 4: 413-418 1996). It has also been demonstrated thatFAK promotes the migration of cells in vitro. Thus, fibroblasts that aredeficient for the expression of FAK (“knockout” mice for FAK) show arounded morphology and deficiencies in cell migration in response tochemotactic signals, and these defects are suppressed by reexpression ofFAK [D J. Sieg et al., J. Cell Science. 112: 2677-91 1999]. Theoverexpression of the C-terminal domain of FAK (FRNK) blocks thestretching of adherent cells and reduces cellular migration in vitro [A.Richardson and J. T. Parsons Nature. 380: 538-540 1996]. Theoverexpression of FAK in CHO or COS cells or in human astrocytoma cellspromotes migration of the cells. The involvement of FAK in promoting theproliferation and migration of cells in numerous cell types in vitrosuggests the potential role of FAK in neoplastic processes. A recentstudy has effectively demonstrated the increase in the proliferation oftumor cells in vivo after induction of the expression of FAK in humanastrocytoma cells [L. A. Cary et al. J. Cell Sci. 109: 1787-94 1996; D.Wang et al. J. Cell Sci. 113: 4221-4230 2000]. Furthermore,immunohistochemical studies on human biopsies have demonstrated that FAKis overexpressed in prostate cancer, breast cancer, thyroid cancer,cancer of the colon, melanoma, brain cancer and lung cancer, the levelof expression of FAK being directly correlated to the tumors having themost aggressive phenotype [T M Weiner et al. Lancet. 342 (8878):1024-1025 1993; Owens et al. Cancer Research. 55: 2752-2755 1995; K.Maung et al. Oncogene 18: 6824-6828 1999; D. Wang et al. J. Cell Sci.113: 4221-4230 2000]. Protein kinase AKT (also known as PKB) andphosphoinositide 3-kinase (PI3K) are involved in a cell signalingpathway that transmits signals from growth factors activating membranereceptors.

This transduction pathway is involved in numerous cellular functions:regulation of apoptosis, control of transcription and translation,glucose metabolism, angiogenesis and mitochondrial integrity. Firstidentified as an important component of insulin-dependent signalingpathways regulating metabolic responses, serine/threonine kinase AKT wasthen identified as a mediator playing a key role in survival inducedwith growth factors. It has been shown that AKT can inhibit death byapoptosis induced by various stimuli, in a certain number of cell typesand tumor cells. In accordance with these findings, it has been shownthat AKT can, by phosphorylation of given serine residues, inactivateBAD, GSK3β, caspase-9, and Forkhead transcription factor, and canactivate IKKalpha and e-NOS. It is interesting to note that the proteinBAD is found hyper-phosphorylated in 11 human tumor cell lines out of 41studied. Furthermore, it has been shown that hypoxia modulates theinduction of VEGF in cells transformed with Ha-ras by activating thePI3K/AKT pathway and by involving the binding sequence of the HIF-1(hypoxia inducible factor-1) transcription factor known as HRE for“hypoxy-responsive element”.

AKT plays a very important role in cancer pathologies. The amplificationand/or overexpression of AKT has been reported in many human tumors, forinstance gastric carcinoma (amplification of AKT1), ovary carcinoma,breast carcinoma or pancreatic carcinoma (amplification andoverexpression of AKT2) and breast carcinomas deficient in estrogenreceptors, and also androgen-independent prostate carcinomas(overexpression of AKT3). Furthermore, AKT is constitutively activatedin all the PTEN (−/−) tumors, the PTEN phosphatase being deleted orinactivated by mutations in many types of tumors, for instancecarcinomas of the ovary, of the prostate, of the endometrium,glioblastomas and melanomas. AKT is also involved in the oncogenicactivation of bcr-abl (references: A. Khawaja, Nature 1999, 401, 33-34;Cardone et al. Nature 1998, 282, 1318-1321; S. Kitada et al., Am. J.Pathol. 1998 January; 152(1): 51-61; N M Mazure et al. Blood 1997, 90,3322-3331; H. Zhong et al. Cancer Res. 2000, 60, 1541-1545).

SUMMARY OF THE INVENTION

The present invention relates to a cyclic urea compound of formula I:

wherein p is 0, 1 or 2,

-   R and R1, which may be identical or different, are O or NH,-   R2 and R3, which may be identical or different, are hydrogen, alkyl,    alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl that are    optionally substituted, or R2 and R3 taken together with the carbon    atom to which they are attached form 3- to 10-membered carbocyclyl    that is optionally being substituted or 3- to 10-membered    heterocyclyl containing one or more hetero atoms chosen from O, S, N    and NR7 that is optionally being substituted,-   A1 is single bond, alkyl, alkenyl or alkynyl,-   Y and Y1, which may be identical or different, are such that one of    Y and Y1 is —OCF₃, —O—F₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅    and —S(O)_(n)-alkyl and the other of Y and Y1 is —OCF₃, —O—F₂—CHF₂,    —O—CHF₂, —O—CH₂—CF₃, SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen,    halogen, hydroxyl, alkoxy, nitro, —CN, —NR5R6, optionally    substituted alkyl, optionally substituted aryl, optionally    substituted heteroaryl, —CF₃, —O-alkenyl, —O-alkynyl, —O-cycloalkyl,    —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl,    —CONR5R6, or free, salified or esterified carboxyl,    or the

that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4,

-   R5 and R6, which may be identical or different, are hydrogen, alkyl,    alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, optionally    substituted aryl or optionally substituted heteroaryl, or R5 and R6    taken together with the nitrogen atom to which they are attached    form 3- to 10-membered heterocyclyl containing one or more hetero    atoms chosen from O, S, N and NR7 that is optionally being    substituted,-   A2, which may be identical to or different from Al, is defined as Al    or is CO or SO₂,-   B2 is saturated or unsaturated, 3- to 10-membered monocyclic or    bicyclic heterocyclyl containing one or more hetero atoms chosen    from O, S, N and NR7 that is optionally substituted with one or more    identical or different substituents defined as Y2,-   R7 is hydrogen, alkyl, cycloalkyl, phenyl, acyl, —S(O)₂Alk,    —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6,-   Y2 is hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,    heterocyclyl, aryl, heteroaryl, —O-alkenyl, —O-alkynyl,    —O-cycloalkyl, —S(O)_(n)-alkyl, —S(O)_(n)-alkenyl,    —S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl, —COOR13, —OCOR13, NR5R6,    CONR5R6, —S(O)_(n)—NR5R6, —NR10-CO—R13, —NR10-SO₂—R13, NH—SO₂—NR5R6,    —NR10-CO—NR5R6, —NR10-CS—NR5R6 or —NR10-COOR13, all of which are    optionally substituted,-   all the alkyl, alkenyl, alkynyl and alkoxy above are linear or    branched and contain not more than 6 carbon atoms,-   all the cycloalkyl and heterocyclyl above contain not more than 7    carbon atoms,-   all the aryl and heteroaryl above contain not more than 10 carbon    atoms,-   all the carbocyclyl, heterocyclyl, alkyl, alkenyl, alkynyl, alkoxy,    cycloalkyl, heterocyclyl, aryl and heteroaryl above, and also the    ring formed by R5 and R6 with the nitrogen atom to which they are    attached, are optionally substituted with one or more substituents,    which may be identical or different, selected from the group    consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro, aryl,    heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12, —C(═O)—NR11R12,    —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9, —N(R10)-C(═O)—NR11R12,    —N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8, —N(R10)-S(O)_(n)—NR11R12 and    —S(O)_(n)—NR11R12,-   all the aryl and heteroaryl above are optionally substituted with    one or more substituents selected from the group consisting of    alkyl, alkoxy and alkylenedioxy,-   all the cyclic radicals above, and also the ring formed by R5 and R6    with the nitrogen atom to which they are attached, are optionally    substituted with one or more substituents selected from the group    consisting of oxo and thioxo,-   n is 0 to 2,-   R8 is alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,    heterocyclylalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl,-   R9 is defined as R8 or is hydrogen,-   R10 is hydrogen or alkyl,-   R11 and R12, which may be identical or different, are hydrogen,    C₃-C₆ cycloalkyl, C₁-C₄ alkyl or phenyl, optionally substituted with    one or more substituents, which may be identical or different,    selected from the group consisting of halogen, cyano, hydroxyl,    alkoxy, —CF₃, nitro, phenyl, and free, salified, esterified or    amidated carboxyl,-   or R11 and R12 taken together with the nitrogen atom to which they    are attached form 5- to 7-membered cyclic radical containing one or    more hetero atoms chosen from O, S, N and NR7, preferably a cyclic    amine, and-   R13, which may be identical to or different to R5 or R6, is defined    as R5 or R6, or racemic, enantiomeric or diastereoisomeric isomer    form of the compound of formula I, addition salt with mineral or    organic acid or with mineral or organic base thereof, with the    proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃ or —S-alk, A2 is single bond or alkyl and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other imidazolylalkyl;-   b) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH);-   c) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)_(n)-alk, A2 is single bond and B2 is an optionally substituted    5- or 6-membered aromatic heterocyclyl, then R2 and R3 are not    selected from the group consisting of hydrogen, alkyl, arylalkyl,    aryl and heteroaryl; or-   d) when p is 0 to 2, R and R1 are oxygen, A1 is single bond, Y and    Y1, which may be identical or different, are one is —SO₂Alk or    SO₂NH₂ and the other is NR5R6, A2 is single bond or alkylene and B2    is optionally substituted 5- to 10-membered heterocyclyl, then R2    and R3 are not both hydrogen.

The invention is also directed to a pharmaceutical compositioncomprising a compound of formula I, method of preparation thereof andmethod for pharmaceutical use of the compound of formula I in a patient.

DETAILED DESCRIPTION OF THE INVENTION

As used above, and throughout the description of the invention, thefollowing terms, unless otherwise indicated, shall be understood to havethe following meanings: —

The term “Hal”, “Halo” or halogen denotes fluorine, chlorine, bromine oriodine atoms.

The term “alkyl”, “alk”, “Alk” or “ALK” denotes a linear or branchedradical containing not more than 12 carbon atoms, chosen from methyl,ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl,pentyl, isopentyl, sec-pentyl, tert-pentyl, neopentyl, hexyl, isohexyl,sec-hexyl, tert-hexyl, heptyl, octyl, nonyl, decyl, undecyl and dodecylradicals, and also the linear or branched positional isomers thereof.

Mention is made more particularly of alkyl radical containing not morethan 6 carbon atoms, and especially methyl, ethyl, propyl, isopropyl,n-butyl, isobutyl, tert-butyl, linear or branched pentyl and linear orbranched hexyl.

The term “alkenyl” denotes a linear or branched radical containing notmore than 12 carbon atoms and preferably 4 carbon atoms, chosen, forexample, from the following values: ethenyl or vinyl, propenyl or allyl,1-propenyl, n-butenyl, i-butenyl, 3-methyl-2-butenyl, n-pentenyl,hexenyl, heptenyl, octenyl, cyclohexylbutenyl and decenyl, and also thelinear or branched positional isomers thereof, more particularly isallyl or butenyl.

The term “alkynyl” denotes a linear or branched radical containing notmore than 12 carbon atoms and preferably 4 carbon atoms, chosen, forexample, from the following values: ethynyl, propynyl or propargyl,butynyl, n-butynyl, i-butynyl, 3-methyl-2-butynyl, pentynyl or hexynyl,and also the linear or branched positional isomers thereof, moreparticularly is propargyl.

The term “alkoxy” denotes a linear or branched radical containing notmore than 12 carbon atoms and preferably 6 carbon atoms chosen, forexample, from methoxy, ethoxy, propoxy, isopropoxy, linear, secondary ortertiary butoxy, pentoxy, hexoxy and heptoxy radicals, and also thelinear or branched positional isomers thereof.

The term “alkoxycarbonyl” or alkyl-O—CO— denotes a linear or branchedradical containing not more than 12 carbon atoms, in which the alkylradical has the meaning given above: examples include methoxycarbonyland ethoxycarbonyl radicals.

The term “alkylenedioxy” or —O-alkylene-O— denotes a linear or branchedradical containing not more than 12 carbon atoms, in which the alkyleneradical has the meaning given above: examples include methylenedioxy andethylenedioxy radicals.

The term “alkylsulfinyl” or alkyl-SO— denotes a linear or branchedradical containing not more than 12 carbon atoms, in which the alkylradical has the meaning given above and preferably contains 4 carbonatoms.

The term “alkylsulfonyl” or alkyl-SO₂— denotes a linear or branchedradical containing not more than 12 carbon atoms, in which the alkylradical has the meaning given above and preferably contains 4 carbonatoms.

The term “alkylsulfonylcarbamoyl” or alkyl-SO₂—NH—C(═O)— denotes alinear or branched radical containing not more than 12 carbon atoms, inwhich the alkyl radical has the meaning given above and preferablycontains 4 carbon atoms.

The term “alkylthio” or alkyl-S— denotes a linear or branched radicalcontaining not more than 12 carbon atoms and especially is methylthio,ethylthio, isopropylthio and heptylthio radicals.

The term “cycloalkyl” denotes a 3- to 10-membered monocyclic or bicycliccarbocyclic or carbocyclyl radical and especially denotes cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl radicals.

The term “—O-cycloalkyl” denotes a radical in which the cycloalkylradical has the meaning given above.

The term “cycloalkenyl” denotes a 3- to 10-membered monocyclic orbicyclic nonaromatic carbocyclic or carbocyclyl radical containing atleast one double bond, and especially denotes cyclobutenyl,cyclopentenyl and cyclohexenyl radicals.

The term “cycloalkylalkyl” denotes a radical in which cycloalkyl andalkyl are chosen from the values indicated above: this radical thusdenotes, for example, cyclopropylmethyl, cyclopentylmethyl,cyclohexylmethyl and cycloheptylmethyl radicals.

The term “acyl” or rad-CO— denotes a linear or branched radicalcontaining not more than 12 carbon atoms, in which the rad is hydrogen,alkyl, cycloalkyl, cycloalkenyl, cycloalkyl, heterocyclyl or arylradical, these radicals having the values indicated above and beingoptionally substituted as indicated: examples include the formyl,acetyl, propionyl, butyryl or benzoyl radicals, valeryl, hexanoyl,acryloyl, crotonoyl or carbamoyl.

The term “acyloxy” means acyl-O— radical in which acyl has the meaninggiven above: examples include acetoxy or propionyloxy radicals.

The term “acylamino” means acyl-NH— radical in which acyl has themeaning given above.

The term “aryl” denotes unsaturated monocyclic radical or unsaturatedradical consisting of fused carbocyclic rings. Examples of such arylradicals that may be mentioned include phenyl or naphthyl radicals.

Mention is made more particularly of the phenyl radical.

The term “arylalkyl” means radical resulting from the combination of theoptionally substituted alkyl radicals mentioned above and the optionallysubstituted aryl radicals also mentioned above: examples include benzyl,phenylethyl, 2-phenethyl, triphenylmethyl or naphthalenemethyl radicals.

The term “heterocyclic” denotes a saturated carbocyclic radical(heterocyclyl) or unsaturated carbocyclic radical (heteroaryl) which isat least 6-membered, interrupted with one or more hetero atoms, whichmay be identical or different, chosen from oxygen, nitrogen and sulfuratoms.

Heterocyclyl radical that may especially be mentioned include dioxolane,dioxane, dithiolane, thiooxolane, thiooxane, oxiranyl, oxolanyl,dioxolanyl, piperazinyl, piperidyl, pyrrolidyl, imidazolidinyl,pyrazolidinyl, morpholinyl, or tetrahydrofuryl, tetrahydrothienyl,chromanyl, dihydrobenzofuranyl, indolinyl, piperidyl, perhydropyranyl,pyrindolinyl, tetrahydroquinolyl, tetrahydroisoquinolyl andthioazolidinyl radicals, all these radicals being optionallysubstituted.

Among the heterocyclyl radical that may especially be mentioned areoptionally substituted piperazinyl, optionally substituted piperidyl,optionally substituted pyrrolidinyl, imidazolidinyl, pyrazolidinyl,morpholinyl and thioazolidinyl radicals: mention may also be made moreparticularly of optionally substituted morpholinyl, pyrrolidyl andpiperazinyl radicals.

The term “heterocyclylalkyl” means radical in which the heterocyclyl andalkyl residues have the above meanings.

Among the 5-membered heteroaryl radicals that may be mentioned are furylradicals such as 2-furyl, thienyl radicals such as 2-thienyl and3-thienyl, and pyrrolyl, diazolyl, thiazolyl, thiadiazolyl,thiatriazolyl, isothiazolyl, oxazolyl, oxadiazolyl, 3- or 4-isoxazolyl,imidazolyl, pyrazolyl and isoxazolyl radicals.

Among the 6-membered heteroaryl radicals that may especially bementioned are pyridyl radicals such as 2-pyridyl, 3-pyridyl and4-pyridyl, and pyrimidyl, pyrimidinyl, pyridazinyl, pyrazinyl andtetrazolyl radicals.

Among the fused heteroaryl radicals containing at least one hetero atomchosen from sulfur, nitrogen and oxygen, examples include benzothienylsuch as 3-benzothienyl, benzofuryl, benzofuranyl, benzopyrrolyl,benzimidazolyl, benzoxazolyl, thionaphthyl, indolyl, purinyl, quinolyl,isoquinolyl and naphthyridinyl.

Among the fused heteroaryl radicals that may be mentioned moreparticularly are benzothienyl, benzofuranyl, indolyl, quinolyl,benzimidazolyl, benzothiazolyl, furyl, imidazolyl, indolizinyl,isoxazolyl, isoquinolyl, isothiazolyl, oxadiazolyl, pyrazinyl,pyridazinyl, pyrazolyl, pyridyl, pyrimidinyl, pyrrolyl, quinazolinyl,1.3.4-thiadiazolyl, thiazolyl and thienyl radicals and triazolyl groups,these radicals optionally being substituted as indicated for theheteroaryl radicals;

The term “cyclic amine” denotes a 3- to 8-membered cycloalkyl radical inwhich one carbon atom is replaced with a nitrogen atom, the cycloalkylradical having the meaning given above and also possibly containing oneor more other hetero atoms chosen from O, S, SO₂, N and NR7 with R7 asdefined above; examples of such cyclic amines that may be mentionedinclude pyrrolidyl, piperidyl, morpholinyl, piperazinyl, indolinyl,pyrindolinyl and tetrahydroquinolyl radicals.

The term “patient” denotes a human being or other mammal.

The term “prodrug” denotes a compound that may be converted in vivo viametabolic mechanisms (such as hydrolysis) into a product of formula I.For example, an ester of a compound of formula I containing a hydroxylgroup may be converted by hydrolysis in vivo into its parent molecule.Alternatively, an ester of a compound of formula I containing a carboxylgroup may be converted by in vivo hydrolysis into its parent molecule.

Examples of esters of the compound of formula I containing a hydroxylgroup that may be mentioned include the acetates, citrates, lactates,tartrates, malonates, oxalates, salicylates, propionates, succinates,fumarates, maleates, methylenebis-β-hydroxynaphthoates, gentisates,isethionates, di-p-tolyltartrates, methanesulfonates, ethanesulfonates,benzenesulfonates, p-toluenesulfonates, cyclohexylsulfamates andquinates.

Esters of products of formula I that are particularly useful, containinga hydroxyl group, may be prepared from acid residues such as thosedescribed by Bundgaard et. al., J. Med. Chem., 1989, 32, page 2503-2507:these esters especially include substituted (aminomethyl)benzoates,dialkylaminomethylbenzoates in which the two alkyl groups may be linkedtogether or may be interrupted with an oxygen atom or with an optionallysubstituted nitrogen atom, i.e., an alkylated nitrogen atom, or(morpholinomethyl)benzoates, e.g., 3- or 4-(morpholinomethyl)benzoates,and (4-alkylpiperazin-1-yl)benzoates, e.g., 3- or4-(4-alkylpiperazin-1-yl)benzoates.

The carboxyl radical of the compound of formula I may be salified oresterified with various groups known to those skilled in the art, amongwhich nonlimiting examples include the following compounds:

-   -   among the salification compounds, mineral bases such as, for        example, one equivalent of sodium, potassium, lithium, calcium,        magnesium or ammonium, or organic bases such as, for example,        methylamine, propylamine, trimethylamine, diethylamine,        triethylamine, N,N-dimethylethanolamine,        tris(hydroxymethyl)aminomethane, ethanolamine, pyridine,        picoline, dicyclohexylamine, morpholine, benzylamine, procaine,        lysine, arginine, histidine or N-methylglucamine;    -   among the esterification compounds, alkyl radicals to form        alkoxycarbonyl groups such as, for example, methoxycarbonyl,        ethoxycarbonyl, tert-butoxycarbonyl or benzyloxycarbonyl, these        alkyl radicals possibly being substituted with radicals chosen,        for example, from halogen atoms and hydroxyl, alkoxy, acyl,        acyloxy, alkylthio, amino or aryl radicals, such as, for        example, in chloromethyl, hydroxypropyl, methoxymethyl,        propionyloxymethyl, methylthiomethyl, dimethylaminoethyl, benzyl        or phenethyl groups.

The term “esterified carboxyl” means, for example, radical such asalkyloxycarbonyl radical, for example methoxycarbonyl, ethoxycarbonyl,propoxycarbonyl, butyl or tertbutyloxycarbonyl, cyclobutyloxycarbonyl,cyclopentyloxycarbonyl or cyclohexyloxycarbonyl.

Mention may also be made of radicals formed with readily cleavable esterresidues, such as methoxymethyl or ethoxymethyl radicals; acyloxyalkylradicals such as pivaloyloxymethyl, pivaloyloxyethyl, acetoxymethyl oracetoxyethyl; alkyloxycarbonyloxyalkyl radicals such asmethoxycarbonyloxy methyl or ethyl radicals, and isopropyloxycarbonyloxymethyl or ethyl radicals.

A list of such ester radicals may be found, for example, in Europeanpatent EP 0 034 536.

The term “amidated carboxyl” means radical of the type —CONR5R6 asdefined above: also intended are the radicals NCOR6R7 in which theradicals R6 and R7, which may be identical or different, are a hydrogenatom or an alkyl radical containing from 1 to 4 carbon atoms such asmethyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl ortert-butyl radicals and especially amino, alkylamino and dialkylaminoradicals.

The term “alkylamino” means linear or branched methylamino, ethylamino,propylamino or butylamino radical. Alkyl radicals containing not morethan 4 carbon atoms are preferred, the alkyl radicals possibly beingchosen from the alkyl radicals mentioned above.

The term “dialkylamino” means, for example, dimethylamino, diethylaminoand methylethylamino radical. As previously, alkyl radicals containingnot more than 4 carbon atoms, chosen from the list indicated above, arepreferred.

The radicals NR5R6 or NR6R7 may also form a heterocyclyl which may ormay not comprise an additional hetero atom. Mention may be made ofpyrrolyl, imidazolyl, indolyl, piperidyl, morpholinyl and piperazinylradicals. The piperidyl, morpholinyl and piperazinyl radicals arepreferred.

The term “salified carboxyl” means the salt formed, for example, withone equivalent of sodium, potassium, lithium, calcium, magnesium orammonium. Mention may also be made of the salts formed with organicbases such as methylamine, propylamine, trimethylamine, diethylamine andtriethylamine. The sodium salt is preferred.

When the compound of formula I comprise an amino radical that may besalified with an acid, it is clearly understood that these acid saltsalso form part of the invention. Mention may be made of the saltsobtained, for example, with hydrochloric acid or methanesulfonic acid.

The addition salts with mineral or organic acids of the compound offormula I may be, for example, the salts formed with hydrochloric acid,hydrobromic acid, hydriodic acid, nitric acid, sulfuric acid, phosphoricacid, propionic acid, acetic acid, trifluoroacetic acid, formic acid,benzoic acid, maleic acid, fumaric acid, succinic acid, tartaric acid,citric acid, oxalic acid, glyoxylic acid, aspartic acid, ascorbic acid,alkylmonosulfonic acids such as, for example, methanesulfonic acid,ethanesulfonic acid or propanesulfonic acid, alkyldisulfonic acids suchas, for example, methanedisulfonic acid or alpha, beta-ethanedisulfonicacid, arylmonosulfonic acids such as benzenesulfonic acid, andaryldisulfonic acids.

It may be recalled that stereoisomerism may be defined in its broadsense as the isomerism of compounds having the same structural formulaebut whose various groups are arranged differently in space, especiallysuch as in monosubstituted cyclohexanes whose substituent may be in anaxial or equatorial position, and the various possible rotationalconformations of ethane derivatives. However, there is another type ofstereoisomerism, due to the different spatial arrangements of fixedsubstituents, either on double bonds or on rings, which is oftenreferred to as geometrical isomerism or cis-trans (E and Z) isomerism.The term “stereoisomer” is used in the present patent application in itsbroadest sense and thus relates to all the compounds indicated above.

EMBODIMENTS

With reference to inventions described herein, below are particularembodiments related thereto.

A particular embodiment according to the invention is the compound offormula I wherein p is 0 to 2,

-   R and R1, which may be identical or different, are O or NH,-   R2 and R3, which may be identical or different, are hydrogen, alkyl,    alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl which are    optionally substituted, or R2 and R3 taken together with the carbon    atom to which they are attached form 3- to 10-membered optionally    substituted carbocyclyl or 3- to 10-membered optionally substituted    heterocyclyl containing one or more hetero atoms chosen from O, S, N    and NR7,-   A1 is single bond, alkyl, allyl or propynyl,-   Y and Y1, which may be identical or different, are such that one    from among Y and Y1 is selected from the group consisting of —OCF₃,    —S(O)_(n)CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6 and    the other of Y and Y1 is selected from the group consisting of these    same definitions and hydrogen, halogen, hydroxyl, alkoxy, —NR5R6,    optionally substituted alkyl, optionally substituted aryl,    optionally substituted heteroaryl, —CF₃, —O-allyl, —O-propynyl,    —O-cycloalkyl, —S(O)_(n)-allyl, —S(O)_(n)-propynyl,    —S(O)_(n)-cycloalkyl, —CONR5R6 and free, salified or esterified    carboxyl,-   wherein R5 and R6, which may be identical or different, are selected    from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl,    cycloalkenyl, heterocyclyl, aryl and heteroaryl, which are    optionally substituted, or R5 and R6 taken together with the    nitrogen atom to which they are attached form 3- to 10-membered    heterocyclyl containing one or more hetero atoms chosen from O, S, N    and NR7, which is optionally substituted,-   A2, which may be identical to or different from Al, is defined as Al    or CO or SO₂,-   B2 is a saturated or unsaturated heterocyclyl containing 1 or more    identical or different hetero atoms chosen from O, S, N and NR7,    optionally substituted with one or more identical or different    substituents chosen from the definition of Y2,-   R7 is hydrogen, alkyl, cycloalkyl, phenyl, acyl, —S(O)₂Alk,    —S(O)₂Aryl, S(O)₂heteroaryl or —S(O)₂NR5R6 radical,-   Y2 is hydrogen, halogen, hydroxyl, alkyl, alkoxy, cycloalkyl,    heterocyclyl, aryl, heteroaryl, —O-allyl, —O-propynyl,    —O-cycloalkyl, —S(O)_(n)-alkyl, —S(O)-allyl, —S(O)-propynyl,    —S(O)_(n)-cycloalkyl, —COOR9, —OCOR8, —NR5R6, —CONR5R6, —S(O)—R5R6,    —NHCOR8, —NH—S(O)_(n)R8, —NH—S(O)_(n)CF₃ or —NH—SO₂—NR5R6, all these    radicals being optionally substituted,-   all the carbocyclyl, heterocyclyl, alkyl, alkenyl, alkynyl, alkoxy,    cycloalkyl, heterocyclyl, aryl and heteroaryl above are optionally    substituted with one or more substituents, which may be identical or    different, selected from the group consisting of halogen, cyano,    hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9,    —C(═O)—R8, —NR11R12,-   —C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,    N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8,    —N(R10)-S(O)_(n)—NR11R12 or —S(O)_(n)—NR11R12, and-   all the aryl and heteroaryl above are optionally substituted with    one or more substituents selected from the group consisting of alkyl    and alkylenedioxy radicals, or-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃ or —S-alk, A2 is single bond or alkyl and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other imidazolylalkyl;-   b) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH);-   c) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)_(n)-alk, A2 is single bond and B2 is an optionally substituted    5- or 6-membered aromatic heterocyclyl, then R2 and R3 are not    selected from the group consisting of hydrogen, alkyl, arylalkyl,    aryl and heteroaryl; or-   d) when p is 0 to 2, R and R1 are oxygen, A1 is single bond, Y and    Y1, which may be identical or different, are one is —SO₂Alk or    SO₂NH₂ and the other is NR5R6, A2 is single bond or alkylene and B2    is optionally substituted 5- to 10-membered heterocyclyl, then R2    and R3 are not both hydrogen.

Another particular embodiment according to the invention is where

-   p is 0 to 2,-   R and R1, which may be identical or different, are O or NH,-   R2 and R3, which may be identical or different, are hydrogen, alkyl,    alkenyl, cycloalkyl, phenyl and heteroaryl, which are optionally    substituted, or R2 and R3 taken together with the carbon atom to    which they are attached form a carbocyclyl or heterocyclyl, these    radicals being 3- to 10-membered and the heterocyclyl contains one    or more hetero atoms chosen from O, S, N and NR7, all these radicals    being optionally substituted,-   A1 is single bond, alkyl, allyl or propynyl,-   Y and Y1, which may be identical or different, are one from among Y    and Y1 is selected from the group consisting of —OCF₃, —S(O)_(n)CF₃,    S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6 and the other from    Y and Y1 is selected from the group consisting of —OCF₃,    —S(O)_(n)CF₃, S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃, —SO₂NR5R6,    hydrogen, halogen, hydroxyl, alkoxy, NR5R6, optionally substituted    alkyl, optionally substituted phenyl, optionally substituted    pyrazolyl and optionally substituted pyridyl,-   R5 and R6, which may be identical or different, are hydrogen, alkyl,    alkenyl, cycloalkyl, heterocyclyl, phenyl or heteroaryl, which are    optionally substituted, or R5 and R6 taken together with the    nitrogen atom to which they are attached form a 3- to 10-membered    heterocyclyl that contains one or more hetero atoms chosen from O,    S, N and NR7, which is optionally substituted,-   A2, which may be identical to or different from Al, is defined as Al    or is CO or SO₂,-   B2 is a saturated or unsaturated 3- to 10-membered heterocyclyl that    contains one or more hetero atoms, which may be identical or    different, chosen from O, S, N and NR7, optionally substituted with    one or more substituents, which may be identical or different    substituents defined as Y2,-   R7 is hydrogen or an alkyl, cycloalkyl or phenyl radical,-   Y2 is hydrogen, halogen, hydroxyl, alkyl, alkoxy, cycloalkyl,    heterocyclyl, phenyl, heteroaryl, —O-cycloalkyl, —S(O)_(n)-alk,    —S(O)_(n)-cycloalkyl, —COOR9, —OCOR8, —NR5R6, —CONR5R6,    S(O)_(n)—R5R6, —NHCOR8 and —NH—S(O)_(n)R8, all these radicals being    optionally substituted,-   all the alkyl, alkenyl, alkynyl and alkoxy radicals above being    linear or branched and contain not more than 6 carbon atoms,-   all the cycloalkyl and heterocyclyl radicals above containing not    more than 7 carbon atoms,-   all the aryl and heteroaryl radicals above containing not more than    10 carbon atoms,-   all the carbocyclic and heterocyclic alkyl, alkenyl, alkynyl,    alkoxy, cycloalkyl, heterocyclyl,-   aryl and heteroaryl radicals above being optionally substituted with    one or more radicals, which may be identical or different, chosen    from halogen atoms and cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl,    heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12, —C(═O)—NR11R12,    —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9, N(R10)-C(═O)—NR11R12,    —N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8, —N(R10)-S(O)_(n)—NR11R12 and    —S(O)_(n)—NR11R12,-   all the aryl and heteroaryl radicals above are optionally    substituted with one or more radicals chosen from alkyl and    alkylenedioxy,-   n is 0 to 2,-   R8 is alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,    heterocyclylalkyl, phenyl or phenylalkyl,-   R9 is defined as R8 or is hydrogen,-   R10 is hydrogen or alkyl, and-   R11 and R12, which may be identical or different, are hydrogen,    C₁-C₄ alkyl and phenyl, which are optionally substituted with one or    more radicals, which may be identical or different, chosen from    halogen, hydroxyl, alkoxy, —CF₃, nitro, phenyl and free, salified,    esterified or amidated carboxyl, or R11 and R12 taken together with    the nitrogen atom to which they are attached form 5- to 7-membered    cyclic radical containing one or more hetero atoms chosen from O, S,    N and NR7, preferably a cyclic amine, or-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃ or —S-alk, A2 is single bond or alkyl and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other imidazolylalkyl;-   b) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH);-   c) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)-alk, A2 is single bond and B2 is an optionally substituted 5-    or 6-membered aromatic heterocyclyl, then R2 and R3 are not selected    from the group consisting of hydrogen, alkyl, arylalkyl, aryl and    heteroaryl; or-   d) when p is 0 to 2, R and R1 are oxygen, A1 is single bond, Y and    Y1, which may be identical or different, are one is —SO₂Alk or    SO₂NH₂ and the other is NR5R6, A2 is single bond or alkylene and B2    is optionally substituted 5- to 10-membered heterocyclyl, then R2    and R3 are not both hydrogen.

A further particular embodiment according to the invention is where Yand Y1, which may be identical or different, are such that one fromamong Y and Y1 is selected from the group consisting of OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —S(O)_(n)CF₃, —S—CF₂—CF₂—CF₃,—S(O)_(n)-alk, —S-Alk-O-Alk, —S-Alk-OH, —S-Alk-CN, —S-Alk-heterocyclyl,—SO₂CHF₂, —SO₂CF₂CF₃, —SO₂NR5R6 and —SF₅, in which Alk is alkylcontaining from 1 to 4 carbon atoms, and the other from among Y and Y1is chosen from the following values: hydrogen, halogen, nitro, —NR5R6,free or esterified carboxyl, and —CONR5R6,

or the

being optionally substituted with one or more alkyl, which arethemselves optionally substituted, or

-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃ or —S-alk, A2 is single bond or alkyl and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other imidazolylalkyl;-   b) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH); or-   c) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)-alk, A2 is single bond and B2 is an optionally substituted 5-    or 6-membered aromatic heterocyclyl, then R2 and R3 are not selected    from the group consisting of hydrogen, alkyl, arylalkyl, aryl and    heteroaryl.

A further particular embodiment according to the invention is where onefrom among Y and Y1 is hydrogen and the other is chosen from —OCF₃,—S(O)CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, or

-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃ or —S-alk, A2 is single bond or alkyl and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other imidazolylalkyl;-   b) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH); or-   c) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)-alk, A2 is single bond and B2 is an optionally substituted 5-    or 6-membered aromatic heterocyclyl, then R2 and R3 are not selected    from the group consisting of hydrogen, alkyl, arylalkyl, aryl and    heteroaryl.

A further particular embodiment according to the invention is where onefrom among Y and Y1 is hydrogen and the other is chosen from—S(O)_(n)CF₃, —SO-Alk, —S(O)₂Alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, or

-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   a) when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —OCF₃, —SO-Alk, —S(O)₂-alk or —SO₂NH₂, A2 is CH₂ and B2 is an    optionally substituted heterocyclyl, then R2 and R3 are not one    hydrogen and the other alkyl optionally interrupted with O, S or    N-alk; always substituted with a hydroxamate (—CO—NHOH); or-   b) when p is 0, R and R1 are oxygen, A1 is a single bond or alkyl, Y    and Y1, which may be identical or different, are at least one is    —S(O)-alk, A2 is single bond and B2 is an optionally substituted 5-    or 6-membered aromatic heterocyclyl, then R2 and R3 are not selected    from the group consisting of hydrogen, alkyl, arylalkyl, aryl and    heteroaryl.

A further particular embodiment according to the invention is where onefrom among Y and Y1 is hydrogen and the other is chosen from —S(O)CF₃,—SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, or

-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof, with the proviso:-   when p is 0, R and R1 are oxygen, A1 is single bond or alkyl, Y and    Y1, which may be identical or different, are such that one is    hydrogen and the other is —SO₂NH₂, A2 is CH₂ and B2 is an optionally    substituted heterocyclyl, then R2 and R3 are not one hydrogen and    the other alkyl optionally interrupted by O, S or N-alk, always    substituted with a hydroxamate (—CO—NHOH).

A further particular embodiment according to the invention is where onefrom among Y and Y1 is hydrogen and the other is chosen from—S(O)_(n)CF₃, —SO₂CHF₂ and —SO₂CF₂CF₃, or

-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof.

A further particular embodiment according to the invention is where

-   all the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl or    heteroaryl defined above are optionally substituted with one or more    radicals, which may be identical or different, chosen from halogen,    cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl, carboxyl which is    free, salified, esterified with an alkyl radical or amidated with    —NR11aR12a, —C(═O)—R9a,-   —NR11aR12a, —C(═O)—NR11aR12a, —N(R10a)-C(═O)—R9a,    —N(R10a)-C(═O)—OR8a,-   —N(R10a)-C(═O)—NR11aR12a, —N(R10a)-S(O)_(n)—R9a, —S(O)_(n)—R9a,-   —N(R10a)-S(O)_(n)—NR11aR12a or —S(O)_(n)—NR11aR12a,-   all the aryl and heteroaryl above furthermore being optionally    substituted with an ethylenedioxy,-   R8a is hydrogen, alkyl, alkenyl, phenyl, phenylalkyl, heteroaryl or    heteroarylalkyl,-   R9a is alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,    heterocyclylalkyl, phenyl, phenylalkyl, heteroaryl or    heteroarylalkyl,-   R10a is hydrogen or alkyl,-   R11a and R12a, which may be identical or different, are hydrogen,    alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, optionally    substituted with one or more substituents, which may be identical or    different, chosen from halogen, hydroxyl, C₁-C₄ alkyl and C₁-C₄    alkoxy, or R11a and R12a taken together with the nitrogen atom to    which they are attached form a cyclic radical chosen from    pyrrolidyl, piperidyl, piperazinyl, morpholinyl, indolinyl,    pyrindolinyl, tetrahydroquinolyl, thiazolidinyl and naphthyridyl, or-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof.

A further particular embodiment according to the invention is where p is0.

A further particular embodiment according to the invention is where p is1.

A further particular embodiment according to the invention is where p is2.

A further particular embodiment according to the invention is where R1is O.

A further particular embodiment according to the invention is where R isO.

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are hydrogen, alkyl,alkenyl, cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, heterocyclyl,heterocyclylalkyl, heteroaryl or heteroarylalkyl, which are optionallysubstituted, or R2 and R3 taken together with the carbon atom to whichthey are attached form 3- to 10-membered carbocyclyl or heterocyclyl,and the heterocyclyl contains one or more hetero atoms chosen from O, S,N and NR7b, all these radicals being optionally substituted,

-   all the above radicals being optionally substituted with one or more    radicals chosen from halogen, cyano, hydroxyl, alkyl and alkoxy    containing 1 to 4 carbon atoms, —CF₃, nitro, phenyl, carboxyl which    is free, salified, esterified with alkyl or amidated with    —NR11bR12b, —C(═O)—R9b, —NR11bR12b and —C(═O)—NR11bR12b,-   R7b is hydrogen, alkyl or phenyl,-   R9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or phenyl,-   R11b and R12b, which may be identical or different, are hydrogen,    alkyl, cycloalkyl or phenyl, or R11b and R12b taken together with    the nitrogen atom to which they are attached form an optionally    substituted piperazinyl.

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are chosen from hydrogen,alkyl, phenylalkyl, pyridylalkyl and benzothienylalkyl, which areoptionally substituted with one or more radicals chosen from halogen,hydroxyl, alkyl and alkoxy containing from one to 4 carbon atoms, or R2and R3 taken together with the carbon atom to which they are attachedform a 3- to 6-membered cycloalkyl or heterocyclyl containing a nitrogenatom.

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are chosen from hydrogen,alkyl, hydroxyalkyl, phenylalkyl, hydroxyphenylalkyl, pyridylalkyl orthienylbenzothienylalkyl, or R2 and R3 taken together with the carbonatom to which they are attached form a cycloalkyl radical containingfrom 3 to 6 carbon atoms or azetidinyl, pyrrolidyl or piperidyl

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are chosen from hydrogen,alkyl, hydroxyalkyl, phenylalkyl and hydroxyphenylalkyl, or R2 and R3taken together with the carbon atom to which they are attached form acycloalkyl containing from 3 to 6 carbon atoms.

A further particular embodiment according to the invention is where onefrom among R2 and R3 is chosen from hydrogen and alkyl, and the otherfrom among R2 and R3 is chosen from among the broadest definitions of R2and R3, or R2 and R3 taken together with the carbon atom to which theyare attached form a cycloalkyl containing from 3 to 6 carbon atoms.

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are hydrogen and alkyl, orR2 and R3 taken together with the carbon atom to which they are attachedform a cycloalkyl containing from 3 to 6 carbon atoms.

A further particular embodiment according to the invention is where R2and R3, which may be identical or different, are hydrogen and methyl, orR2 and R3 taken together with the carbon atom to which they are attachedform cyclopropyl.

A further particular embodiment according to the invention is where A1is single bond and A2 is chosen from single bond, a linear or branchedalkyl containing not more than 6 carbon atoms and allyl, propynyl, C═Oand SO₂ radicals, the other substituents of said compound of formula Ihaving any one of the values defined above.

A further particular embodiment according to the invention is where A1is single bond and A2 is chosen from single bond, alkyl, allyl,propynyl, C═O and SO₂.

A further particular embodiment according to the invention is where A1is single bond and A2 is chosen from alkyl, allyl, propynyl, C═O andSO₂.

A further particular embodiment according to the invention is where A1is single bond and A2 is alkyl or C═O.

A further particular embodiment according to the invention is where A1is single bond and A2 is C═O, ethylene or methylene.

A further particular embodiment according to the invention is where A1is single bond and A2 is methylene.

A further particular embodiment according to the invention is where Yand Y1 are such that one is hydrogen, halogen or amino and the other ischosen from —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SF₅,—S(O)_(n)—CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃, —SO₂NH₂,—S—CF₂—CF₂—CF₃, —S-Alk-O-Alk, —S-Alk-OH, —S-Alk-CN, —S-Alk-morpholino,—S-Alk-pyrrolidinyl and —S-Alk-piperazinyl, wherein the morpholino,pyrrolidinyl and piperazinyl are optionally substituted with Alk, inwhich Alk is alkyl containing from 1 to 4 carbon atoms.

A further particular embodiment according to the invention is where Y ishydrogen and Y1 is chosen from —OCF₃, S(O)_(n)—CF₃, —S(O)_(n)—CH₃,—SO₂CHF₂ and —SO₂NH₂.

A further particular embodiment according to the invention is where Y ishydrogen and Y1 is chosen from —OCF₃, —S(O)_(n)—CF₃ and —SO₂CHF₂.

A further particular embodiment according to the invention is where Y ishydrogen and Y1 is chosen from —OCF₃ and S(O)_(n)—CF₃.

A further particular embodiment according to the invention is where Y ishydrogen and Y1 is chosen from —OCF₃, S—CF₃ and S(O)₂—CF₃.

A further particular embodiment according to the invention is where B2is monocyclic or bicyclic heteroaryl chosen from pyridyl, pyrimidinyl,quinolyl, azaindolyl, 1H-pyrrolo[2,3-b]pyridinyl, quinazolyl, thiazolyl,imidazolyl, pyrazolyl, furazanyl, isoxazolyl, morpholinyl, pyrrolidinyl,furyl, piperidyl, thienyl, chromenyl, oxochromenyl, indolyl, pyrrolyl,purinyl, benzoxazinyl, benzimidazolyl and benzofuranyl, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.

A further particular embodiment according to the invention is where B2is heteroaryl chosen from 3- or 4-pyridyl, 3- or 4-quinolyl, imidazolyl,thiazolyl, indolyl, pyrazolyl, pyrrolyl, pyrimidyl, purinyl,benzoxazinyl, benzimidazolyl and benzofuranyl, which are optionallysubstituted with one or more radicals chosen from the definition of Y2.

A further particular embodiment according to the invention is where B2is heteroaryl chosen from 4-pyridyl, 4-quinolyl, imidazolyl, thiazolyl,pyrazolyl, pyrrolyl, pyrimidyl and purinyl radicals, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.

A further particular embodiment according to the invention is where B2is heteroaryl chosen from 3- or 4-pyridyl, pyrimidinyl, 3- or4-quinolyl, azaindolyl, quinazolyl, thiazolyl, imidazolyl, pyrazolyl,furazanyl and isoxazolyl, which are optionally substituted with one ormore radicals chosen from the definition of Y2.

A further particular embodiment according to the invention is where B2is heteroaryl chosen from 3- or 4-pyridyl, pyrimidyl, 3- or 4-quinolyl,azaindolyl and quinazolyl, which are optionally substituted with one ormore radicals chosen from the definition of Y2.

A further particular embodiment according to the invention is where B2is 4-pyridyl, 4-quinolyl or 1H-pyrrolo[2,3-b]pyrid-4-yl, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.

A further particular embodiment according to the invention is where Y2is 2-amino-4-pyridyl in which the amino is optionally substituted asindicated for the radical —NR5R6 as defined herein and in theexperimental section.

A further particular embodiment according to the invention is where Y2is hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, phenyl, —COOH,—COOAlk, —CONR5R6, —NR5R6, —NR10-COOR6, —NR10-CO—R6, —NR10-CS—NR5R6,—NR10-CO—NR5R6 or —NR10-SO₂—R6, which are all optionally substituted,

-   R5 and R6, which may be identical or different, are chosen from    hydrogen, alkyl, cycloalkyl, phenyl and 5- or 6-membered heteroaryl    containing 1 to 3 hetero atoms chosen from O, N and S, which are all    optionally substituted, or R5 and R6 taken together with the    nitrogen atom to which they are attached form an optionally    substituted pyrrolidinyl, piperidyl, piperazinyl, morpholinyl or    quinazolinyl,-   R10 is hydrogen or alkyl,-   all the alkyl, alkoxy, cycloalkyl and phenyl, and also the ring    formed by R5 and R6 with the atom to which they are attached, are    optionally substituted with one or more radicals, which may be    identical or different, chosen from halogen, cyano, hydroxyl, alkyl,    alkoxy, OCF₃, —CF₃, —S(O)_(n)—CF₃, nitro, oxo, thioxo, —OCOAlk; and    phenyl, which is optionally substituted with one or more radicals    chosen from halogen, alkyl, alkoxy; —OCOAlk; —NH₂, —NHAlk, —N(Alk)₂,    —N(alk)(phenylalkyl), —N(Alk)(aminoalkyl), —N(Alk)(alkylaminoalkyl),    —N(Alk)(dialkylaminoalkyl), and carboxyl in free form or esterified    with an alkyl,-   all phenyl herein are optionally substituted with alkylenedioxy,-   all alkyl herein are optionally substituted with one or more    saturated or partially unsaturated 4- to 7-membered heterocyclyl    containing at least one nitrogen atom N and 0 to 2 other hetero    atoms chosen from O, N and S,-   all the pyrrolidinyl and quinazolinyl herein are optionally    substituted with oxo or thioxo,-   all the alkyl and alkoxy herein being linear or branched and    containing not more than 6 carbon atoms,-   all the cycloalkyl herein containing not more than 7 carbon atoms.

A further particular embodiment according to the invention is where R5and R6 represent pyridyl, pyrazinyl, pyrimidinyl, thienyl, thiazolyl andoxazolyl, which are all optionally substituted.

A further particular embodiment according to the invention is where thealkyl is optionally substituted with heterocyclyl chosen fromthiomorpholin-4-yl, thiazolidin-3-yl, azetidin-1-yl, piperazinyl,imidazolyl, morpholinyl, pyrrolidinyl, piperidyl and azepanyl, all ofwhich are optionally substituted as indicated herein; especially withone or more radicals chosen from alkyl, hydroxyalkyl, oxo, pyridyl andphenyl optionally substituted with one or more radicals chosen fromhalogen, alkyl, hydroxyl, alkoxy, —CN, carboxyl or amino, which arethemselves optionally substituted.

Examples include piperazinyl optionally substituted with Alk, Alk-OH,pyridyl or phenyl, which itself is optionally substituted with one ormore radicals chosen from halogen, alkyl, hydroxyl, alkoxy, —CN,carboxyl and amino, which are themselves optionally substituted;piperidyl optionally substituted with one or two Alk; or azepanyloptionally substituted with oxo.

-   Y2 is hydrogen, halogen, hydroxyl, cyano, alkyul, alkoxy, phenyl,    —CONR5R6, —NR5R6, —NR10-COOH, —NR10-COOAlk, —NR10-CO—R6,    —NR10-CS—NR5R6, —NR10-CO—NR5R6 or —NR10-SO₂—R6,-   R5 and R6, which may be identical or different, are chosen from    hydrogen; alkyl; cycloalkyl; phenyl; pyrimidinyl; thienyl; pyridyl;    quinolyl; thiazolyl optionally substituted with one or two halogen;    pyran optionally substituted with one or more —OCOAlk; phenyl    substituted with one or more radicals chosen from halogen, alkyl,    alkoxy, amino, alkylamino, dialkylamino and carboxyl in free form or    esterified with an alkyl radical; alkyl substituted with phenyl,    which is itself optionally substituted with one or more radicals    chosen from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino,    carboxyl in free form or esterified with an alkyl radical; alkyl    substituted with piperazinyl, which is itself optionally substituted    with one or more radicals chosen from Alk, Alk-OH and pyridyl; alkyl    substituted with imidazolyl; alkyl substituted with one or more    radicals chosen from —NH₂, —NHAlk, —N(Alk)₂, —N(alk)(phenylalkyl),    —N(Alk)(aminoalkyl), —N(Alk)(alkylaminoalkyl) and    —N(Alk)(dialkylaminoalkyl); alkyl substituted with morpholinyl    optionally substituted with one or two Alk; alkyl substituted with    pyrrolidinyl; alkyl substituted with piperidyl, which is itself    optionally substituted with one or two Alk; alkyl substituted with    thiomorpholinyl; alkyl substituted with azetidinyl; and alkyl    substituted with azepanyl, which is optionally substituted with oxo,-   or R5 and R6 taken together with the nitrogen atom to which they are    attached form pyrrolidinyl; piperidyl; piperazinyl; morpholinyl; or    quinazolinyl, all of which are optionally substituted with one or    more radicals, which may be identical or different, chosen from    halogen, alkyl, hydroxyl and alkoxy, and phenyl which is optionally    substituted with one or more radicals chosen from halogen, alkyl and    alkoxy,-   pyrrolidinyl and quinazolinyl are optionally substituted with oxo or    thioxo,-   the piperazinyl itself is optionally substituted with one or more    radicals chosen from Alk, Alk-OH and pyridyl,-   R10 is hydrogen or alkyl,-   all alkyl, Alk and alkoxy above being linear or branched and    containing not more than 6 carbon atoms,-   all the cycloalkyl herein containing not more than 7 carbon atoms,-   all the phenyl are optionally substituted with a radical chosen from    —CF₃, —OCF₃, nitro and alkylenedioxy.

Further particular embodiments according to the invention are directedto the three structures below, in which the definition of —NR14R15 ischosen from the definition of

—NR5R6 and the definition for Alkyl, Aryl and Heteroaryl are chosen fromthe values of the alkyl, aryl and heteroaryl as defined above andoptionally substituted as defined herein.

A further particular embodiment according to the invention is where B2is the 4-pyridyl and 4-quinolyl, which are optionally substituted withone or more radicals chosen from the definition of Y2.

A further particular embodiment according to the invention is where Y2is VI, halogen, hydroxyl, —C(═NH)NH₂, OV1, O—CO—V1, COOV1, COV1,CO—NV1V2, —NV1V2, —NH—CO—V1, —NH—COO—V1, —NH—NH—CO—V1, —NV1-CO—NV1V2,—NV1-CO—NHV1, —NH—CO—NHV1, —NH—SO₂—NHV1 and —NH—SO₂—V1, in which V1 andV2, which may be identical or different, are hydrogen, alkyl, cycloalkylor phenyl or heterocyclyl such as pyridyl, pyrazolyl, imidazolyl,dihydroimidazolyl, tetrazolyl, morpholinyl, piperazinyl,piperazinylalkyl, alkylpiperazinyl, phenylpiperazinyl, thienyl, furanyl,piperidyl, methylpiperidyl, pyridyl, pyrrolidyl and pyrrolidylalkyl,

-   all the alkyl, phenyl and heterocyclyl being optionally substituted    with one or more radicals chosen from halogen, hydroxyl, alkyl,    alkoxy, —CF₃, NH₂, NH-alk, N(Alk)₂ and phenyl, itself optionally    substituted with one or more substituents chosen from halogen,    hydroxyl and alkoxy radicals,-   all the phenyl and heterocyclyl herein are optionally substituted    with one or more alkyl, the phenyl is optionally substituted with    —NR5R6 in which R5 and R6 are as defined herein.

A further particular embodiment according to the invention is where Y2is hydrogen, halogen, alkyl, cycloalkyl, hydroxyl, alkoxy, carboxylwhich is free or esterified with an alkyl or phenyl, —NH₂, —NHalk,—N(Alk)₂ or phenyl,

-   all the alkyl, alkoxy and phenyl are optionally substituted with one    or more radicals chosen from halogen, hydroxyl, C₁-C₄ alkyl, C₁-C₄    alkoxy, —CF₃, —NH₂, —NH-alk, N(Alk)₂ and phenyl, which is itself    optionally substituted with one or more substituents chosen from    halogen, hydroxyl and alkoxy,-   all the phenyl are optionally substituted with one or more C₁-C₄    alkyl and optionally substituted with —NR5R6 in which R5 and R6 are    as defined herein.

A further particular embodiment according to the invention is where Y2is hydrogen, F, Cl, —CH₃, —CH₂CH₃, —OH, —OCH₃, —NH₂, —NH-Alk and phenyloptionally substituted with —NR5R6 in which R5 and R6 are as definedherein.

A further particular embodiment according to the invention is where B2is 4-pyridyl and 4-quinolyl substituted with one or two radicals chosenfrom F, Cl, —OH and —OCH₃.

A further particular embodiment according to the invention is where

is which is selected from the following

A further particular embodiment according to the invention is where-A2-B2-Y2 are selected from the following radicals:

A further particular embodiment according to the invention is where R2and R3 form together a cycloalkyl or heterocyclyl, or identical ordifferent, are hydrogen or methyl.

A further particular embodiment according to the invention correspondingto formula (IC):

in which YC and Y1C are such that one is hydrogen, halogen, or amino andthe other is chosen from —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SF₅,—S(O)_(n)—CF₃, —S(O)_(n)-alk, —SO₂CHF₂, SO₂CF₂CF₃, —SO₂NH₂,—S—CF₂—CF₂—CF₃, —S-Alk-O-Alk, —S-Alk-OH, —S-Alk-CN, —S-Alk-morpholino,—S-Alk-pyrrolidyl and —S-Alk-piperazinyl, the morpholino, pyrrolidyl andpiperazinyl are optionally substituted with Alk, with Alk being alkylcontaining from 1 to 4 carbon atoms,

-   or the phenyl thereof with its substituents YC and Y1C forms one of    the two following radicals:

R2C and R3C, which may be identical or different, are hydrogen oroptionally substituted alkyl, or R2C and R3C taken together with thecarbon atom to which they are attached form a C₃-C₁₀ cycloalkyl orheterocyclyl,

-   A2C is single bond or CH₂,-   B2C is pyridyl, pyrimidyl, quinolyl, azaindolyl, quinazolyl,    thiazolyl, imidazolyl, pyrazolyl, furazanyl, isoxazolyl,    morpholinyl, pyrrolidyl, furyl, piperidyl, chromenyl, oxochromenyl,    quinazolyl, thienyl, indolyl, pyrrolyl, purinyl, benzoxazinyl,    benzimidazolyl or benzofuryl, that are optionally substituted with    one or more radicals chosen from the definition of Y2A, Y2CA is    hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, phenyl, —COOH,    —COOAlk, —CONR5R6, —NR5R6, —NR10-COOH, —NR10-COOAlk, —NR10-CO—R6,    —NR10-CS—NR5R6, —NR10-CO—NR5R6 or —NR10-SO₂—R6, all these radicals    are optionally substituted,-   R5 and R6, which may be identical or different, are chosen from    hydrogen, alkyl, cycloalkyl, phenyl, pyrimidyl, thienyl, pyridyl,    quinolyl, thiazolyl and pyran, all these radicals are optionally    substituted, or R5 and R6 taken together with the nitrogen atom to    which they are attached form optionally substituted pyrrolidyl,    piperidyl, piperazinyl, morpholinyl or quinazolinyl,-   R10 is hydrogen or alkyl,-   all the alkyl, Alk or ALK, alkoxy, cycloalkyl and phenyl radicals    herein, and also the ring formed by R5 and R6 with the atom to which    they are attached, are optionally substituted with one or more    radicals, which may be identical or different, chosen from halogen,    cyano, hydroxyl, alkyl, alkoxy, —OCF₃, —CF₃, —S(O)_(n)—CF₃, nitro,    oxo, thioxo, —OCOAlk, and phenyl, itself optionally substituted with    one or more radicals chosen from halogen, alkyl, alkoxy;-   —OCOAlk; —NH₂, —NHAlk, —N(Alk)₂, —N(alk)(phenylalkyl),    —N(Alk)(aminoalkyl) —N(Alk)(alkylaminoalkyl),    —N(Alk)(dialkylaminoalkyl); carboxyl in free form or esterified with    alkyl,-   all the phenyl herein are optionally substituted with alkylenedioxy,-   all the alkyl herein are optionally substituted with one or more    radicals chosen from piperazinyl, itself optionally substituted with    Alk, Alk-OH and pyridyl; imidazolyl; morpholinyl; pyrrolidyl;    piperidyl, itself optionally substituted with one or two alk;    azepanyl optionally substituted with oxo,-   all the pyrrolidyl and quinazolinyl herein are optionally    substituted with oxo or thioxo,-   all the alkyl and alkoxy herein being linear or branched and    containing not more than 6 carbon atoms,-   all the cycloalkyl herein containing not more than 7 carbon atoms,    and-   n is 0 to 2, or-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof.

A further particular embodiment according to the invention is where, theradical below that can be formed by phenyl with its substituents Y andY1:

A further particular embodiment according to the invention correspondsto formula (IA):

in which:

-   Y1A is —OCF₃, —S(O)_(n)—CF₃ and —SO₂CHF₂,-   B2a is 4-quinolyl and 4-pyridyl optionally substituted with one or    more radicals chosen from the definition of Y2A,-   Y2A is defined as Y2,-   R2A and R3A, which may be identical or different, are hydrogen or    optionally substituted alkyl, or R2A and R3A taken together with the    carbon atom to which they are attached form a C₃-C₁₀ cycloalkyl or    heterocyclyl,-   all the alkyl and phenyl are optionally substituted with one or more    radicals chosen from halogen, —OH, alk, —O-alk, —OCF₃,    —S(O)_(n)—CF₃, —CF₃, —NH₂, —NH-Alk and —N(Alk)₂, and-   n is 0 to 2, or-   racemic, enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof.

A further particular embodiment according to the invention is for thecompound of formula (IA) as defined above in which Y1A, B2a, R2A and R3Ahave the meanings given above and Y2A is halogen, —OH, -alk, —Oalk,—Oacyl, —NR5AR6A, —CO₂H, —CO₂alk, —CO-1—NR5AR6A, —S(O)_(n)—CF₃,—NH—S(O)_(n)—CF₃ or phenyl, alk is a linear or branched alkyl radicalcontaining not more than 6 carbon atoms, all the alkyl, alkoxy andphenyl are optionally substituted,

-   R5A and R6A, which may be identical or different, are hydrogen,    alkyl, cycloalkyl or phenyl, the alkyl and phenyl are optionally    substituted, or R5A and R6A taken together with the nitrogen atom to    which they are attached form cyclic radical chosen from pyrrolidyl,    piperidyl, piperazinyl, morpholinyl, indolinyl, pyrindolinyl,    tetrahydroquinolyl and azetidinyl,-   all the alkyl, alkoxy and phenyl are optionally substituted with one    or more radicals chosen from halogen, —OH, alk, —Oalk, —OCF₃,    —S(O)_(n)—CF₃, —CF₃, —NH₂, —NH-Alk and —N(Alk)₂, and n is 0 to 2, or-   said products of formula (IA) being in any possible racemic,    enantiomeric or diastereoisomeric isomer form, and also the addition    salts with mineral and organic acids or with mineral and organic    bases of said products of formula (IA).

A subject of the present invention is especially the compound of formula(IA) as defined above in which:

-   Y1A is —OCF₃, SCF₃ or S(O)₂—CF₃,-   B2a is a 4-quinolyl or 4-pyridyl radical optionally substituted with    one or two radicals chosen from halogen, —OH, alk, —Oalk, —CO₂H,    —CO₂alk, —NR5AR6A, —CF₃, —OCF₃ and optionally substituted phenyl,-   R5A and R6A, which may be identical or different, are hydrogen,    alkyl, cycloalkyl or phenyl, the alkyl and phenyl radicals being    optionally substituted,-   or R5A and R6A taken together with the nitrogen atom to which they    are attached form a cyclic radical chosen from pyrrolidyl,    piperidyl, piperazinyl, morpholinyl, piperazinyl and azetidinyl    radicals,-   R2A and R3A, which may be identical or different, are hydrogen or    optionally substituted alkyl, or R2A and R3A taken together with the    carbon atom to which they are attached form a C₃-C₆ cycloalkyl or    heterocyclyl radical,-   all the alkyl and phenyl radicals being optionally substituted with    one or more radicals chosen from halogen, OH, alk, Oalk, OCF₃,    S(O)_(n)—CF₃, —CF₃, NH₂, NHalk and N(Alk)₂, said products of formula    (IA) being in any possible racemic, enantiomeric or racemic,    enantiomeric or diastereoisomeric isomer form of the compound of    formula I, addition salt with mineral or organic acid or with    mineral or organic base thereof.

A subject of the present invention is especially the compound of formula(IA) as defined above corresponding to formula (IA) in which:

-   Y1A is —OCF₃, —SCF₃ or —S(O)₂—CF₃,-   B2a is 4-quinolyl or 4-pyridyl optionally substituted with one or    two radicals chosen from halogen, —OH, alk and —Oalk, and-   R2A and R3A, which may be identical or different, are hydrogen or    linear or branched alkyl containing not more than 4 carbon atoms    optionally substituted with hydroxyl, or R2A and R3A taken together    with the carbon atom to which they are attached form a C₃-C₆    cycloalkyl, or-   said products of formula (IA) being in any possible racemic,    enantiomeric or enantiomeric or diastereoisomeric isomer form of the    compound of formula I, addition salt with mineral or organic acid or    with mineral or organic base thereof.

A subject of the present invention is especially the compound of formula(IA) as defined above corresponding to formula (IA) in which Y1a is—OCF₃, —SCF₃ or —S(O)₂CF₃, and R2A and R3A, which may be identical ordifferent, are hydrogen or CH₃, or R2A and R3A taken together with thecarbon atom to which they are attached form cyclopropyl, ordiastereoisomeric isomer form of the compound of formula I, additionsalt with mineral or organic acid or with mineral or organic basethereof.

A subject of the present invention is especially the compound of formula(I) as defined above corresponding to formula (IB):

in which R2, R3, A1, Y, Y1, A2, B2 and Y2 have the meanings given aboveor diastereoisomeric isomer form of the compound of formula I, additionsalt with mineral or organic acid or with mineral or organic basethereof.

-   A subject of the present invention is especially the compound of    formula (IB) as defined above in which Y1 is —OCF₃, —SCF₃ or    —S(O)₂CF₃ and R2 and R3, which may be identical or different, are    hydrogen or —CH₃, or R2 and R3 taken together with the carbon atom    to which they are attached form cyclopropyl, or-   diastereoisomeric isomer form of the compound of formula I, addition    salt with mineral or organic acid or with mineral or organic base    thereof.

Among the compounds of the invention that are preferred, are givenbelow:

-   (S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (S)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethane-sulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-4-methyl-3-quinol-4-ylmethyl-5-thioxo-1-(4-trifluoromethylsulfanylphenyl)imidazolidin-2-one    trifluoroacetate;-   (R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(4-hydroxybenzyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(4-hydroxybenzyl)-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(1-hydroxyethyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-pyrid-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   (R)-1-(3-hydroxypyrid-4-ylmethyl)-5-methyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate, said compound of formula I being in any possible    racemic, enantiomeric or diastereoisomeric isomer form, and also the    addition salts with mineral and organic acids or with mineral and    organic bases of said compound of formula I.    Among the preferred products of the invention, mention may be made    more particularly of the compound of formula I as defined above, the    names of which are given below:-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}cyclopropanecarboxamide    trifluoroacetate;-   5,5-dimethyl-1-[2-(pyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)-imidazolidine-2,4-dione;    compound with trifluoroacetic acid;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}    isobutyramide; compound with trifluoroacetic acid;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;    compound with trifluoroacetic acid;-   1-(2-aminopyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    hydrochloride;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}pyridine-2-carboxamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-piperid-1-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-[4-(2-hydroxyethyl)piperazin-1-yl]propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-morpholin-4-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-pyrrolidin-1-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-methylpiperazin-1-yl)propionamide    trifluoroacetate;-   1-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-phenylurea;-   1-[2-(6-ethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(6-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imi-dazolidine-2,4-dione;-   1-[2-(4,6-dimethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(3,5-dichloropyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(pyrid-4-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(pyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2-oxoazepan-1-yl)propionamide;-   3-(benzylmethylamino)-N-{4-[5,5-dimethyl-2,4-di-oxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   4,5-diacetoxy-6-acetoxymethyl-2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureidoacetic    acid;-   5,5-dimethyl-1-[2-(5-methylpyrid-2-ylamino)pyri-din-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3,5-dimethoxybenzamide    trifluoroacetate;-   5,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3-methylpiperid-1-yl)propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3,5-dimethylpiperid-1-yl)propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-methoxybenzamide    trifluoroacetate;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}pyrazine-2-carboxamide    trifluoroacetate;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thiophene-2-carboxamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-4-methylbenzamide;    compound with trifluoroacetic acid;-   1-isoquinolin-5-yl-5,5-dimethyl-3-(4-trifluoro-methylsulfanylphenyl)imidazolidine-2,4-dione;-   3-(4-acetylpiperazin-1-yl)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   3-[4-(2-diethylaminoethyl)piperazin-1-yl]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2,6-dimethylmorpholin-4-yl)propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-pyrrolidin-1-ylpiperid-1-yl)propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-(4-pyrrolidin-1-ylpiperid-1-yl)acetamide;-   5,5-dimethyl-1-[2-(4-methylpyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(6-morpholin-4-ylpyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2,6-dimethylpyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   methyl    5-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-ylamino}pyridine-2-carboxylate;-   1-[2-(2,6-dimethoxypyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(6-fluoropyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(6-methoxypyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione,    said compound of formula I being in any possible racemic,    enantiomeric or diastereoisomeric isomer form, and also the addition    salts with mineral and organic acids or with mineral and organic    bases of said compound of formula I.-   A subject of the present invention is also a process for preparing    the compound of formula I as defined above, characterized in that:-   either a product of formula (II):

in which Y′ and Y1′ have the meanings given above for Y and Y1,respectively, in which the optional reactive functions are optionallyprotected and R has the meaning given above, is reacted in the presenceof a tertiary base with a product of formula (III):

in which X is -A2′-B2′-Y2′ or hydrogen, and A2′, B2′, Y2′, R2′ and R3′have the meanings given above, respectively, for A2′, B2′, Y2′, R2′ andR3′ in which the optional reactive functions are optionally protectedabove, to obtain a product of formula (IV):

in which Y′, Y1′, X, R, R2′ and R3′ have the meanings given above,

-   which products of formula (IV) are, if necessary or if desired,    subjected to any one or more of the following reactions, in any    order:-   a) reaction for removal of any protecting groups that may be borne    by Y′, Y1′, R, R2′ and R3′ and X when X is -A2′-B2′-Y2′;-   b) reaction for hydrolysis of the >C═NH group to a ketone function-   c) action on the products of formula (IV) in which X is hydrogen,    and after optional hydrolysis of the >C═NH group to a ketone    function of a reagent of formula Hal-A2′-B2′-Y2′ in which A2′, B2′    and Y2′ have the meanings given above and Hal is a halogen atom, to    obtain products of formula (Ii):

in which Y′, Y1′, R2′, R3′, A2′, B2′ and Y2′ have the meanings givenabove, followed, if desired, by the action on these products of an agentfor removing any protecting groups that may be borne by Y′, Y1′, R2′,R3′, A2′, B2′ and Y2′ or, where appropriate, the action of anesterification, amidation or salification agent,

-   or the product of formula (II) defined above is reacted in the    presence of a tertiary base with a product of formula (III′):

in which R2′ and R3′ have the meanings given above and Q is either analkali metal atom, for example sodium, or an alkyl radical containingfrom 1 to 6 carbon atoms, to obtain a product of formula (IVa):

in which Y′, Y1′, R, R2′, R3′ and X have the meanings given above, whichproduct, if desired, is subjected to any one or more of the followingreactions, in any order:

-   a) reaction for removal of the possible protecting groups that may    be borne by X;-   b) action on the products of formula (IVa), in which X is hydrogen,    of a reagent of formula Hal-A2′-B2′-Y2′ in which A2′, B2′ and Y2′    have the meanings given above and Hal is a halogen atom, to obtain    products of formula (iii):

in which Y′, Y1′, R, R1, R2′, R3′ and A2′, B2′ and Y2′ have the meaningsgiven above, followed, if desired, by the action on these products of anagent for removing any protecting groups that may be borne by Y′, Y1′,R2′, R3′, A2′, B2′ and Y2′ or, where appropriate, the action of anesterification, amidation or salification agent,

-   or a reagent of formula Hal-A2′-B2′-Y2′, in which A2′, B2′, Y2′ and    Hal have the meanings given above, is reacted with a product of    formula (IV′):

in which Y′, Y1′, R2′ and R3′ have the meanings given above, to obtain aproduct of formula (IV″):

in which Y′, Y1′, R2′, R3′, A2′, B2′ and Y2′ have the meanings givenabove, which product of formula (IV″) is, if necessary or if desired,subjected to a reaction for removal of any protecting groups that may beborne by -A2′-B2′-Y2′, followed, where appropriate, by the action of anesterification, amidation or salification agent.

It may be noted that, depending on the values of Y′, Y1′, R2′, R3′, A2′,B2′ and Y2′, the products of formulae (IV), (Ii), (IVa), (Iii) and (IV″)may be compound of formula I and that, to obtain products or othercompound of formula I, these products may be subjected if desired, andnecessary, to one or more of the following conversion reactions, in anyorder:

-   a) a reaction for esterification of an acid function,-   b) a reaction for saponification of an ester function to an acid    function,-   c) a reaction for oxidation of an alkylthio group to the    corresponding sulfoxide or sulfone group,-   d) a reaction for conversion of a ketone function to an oxime    function,-   e) a reaction for reducing a free or esterified carboxyl function to    an alcohol function,-   f) a reaction for conversion of an alkoxy function to a hydroxyl    function, or of a hydroxyl function to an alkoxy function,-   g) a reaction for oxidation of an alcohol function to an aldehyde,    acid or ketone function,-   h) a reaction for conversion of a nitrile radical to a tetrazolyl,-   i) a reaction for reduction of nitro compounds to amino compounds,-   j) a reaction for removal of the protecting groups that may be borne    by the protected reactive functions,-   k) a reaction for salification with a mineral or organic acid or    with a base to obtain the corresponding salt,-   l) a reaction for resolution of the racemic forms to resolved    products, said compound of formula I thus obtained being in any    possible racemic, enantiomeric or diastereoisomeric isomer form.

It may be noted that such reactions for converting substituents intoother substituents may also be performed on the starting materials, andalso on the intermediates as defined above before continuing thesynthesis according to the reactions indicated in the process describedabove.

The various reactive functions that may be borne by certain compounds ofthe reactions defined above may, if necessary, be protected: these are,for example, hydroxyl, acyl, free carboxyl or amino and monoalkylaminoradicals, which may be protected with the appropriate protecting groups.

The following nonexhaustive list of examples of protection of reactivefunctions may be mentioned:

The hydroxyl groups may be protected, for example, with alkyl radicalssuch as tert-butyl, trimethylsilyl, tert-butyldimethylsilyl,methoxymethyl, tetrahydropyranyl, benzyl or acetyl.

The amino groups may be protected, for example, with acetyl, trityl,benzyl, tert-butoxycarbonyl, benzyloxycarbonyl, phthalimido radicals orother radicals known in peptide chemistry.

The acyl groups such as the formyl group may be protected, for example,in the form of cyclic or noncyclic ketals or thioketals such as dimethylor diethylketal or ethylene dioxyketal, or diethylthioketal orethylenedithioketal.

The acid functions of the products described above may be, if desired,amidated with a primary or secondary amine, for example in methylenechloride in the presence, for example, of1-ethyl-3-(dimethylaminopropyl)carbodiimide hydrochloride at roomtemperature.

The acid functions may be protected, for example, in the form of estersformed with readily cleavable esters such as benzyl esters or tert-butylesters, or esters known in peptide chemistry.

These reactions a) to k) indicated above may be performed, for example,as indicated below.

-   a) The products described above may, if desired, undergo, on the    possible carboxyl functions, esterification reactions that may be    performed according to the usual methods known to those skilled in    the art.-   b) The possible conversions of ester functions into an acid function    of the products described above may be, if desired, performed under    the usual conditions known to those skilled in the art, especially    by acid or alkaline hydrolysis, for example with sodium hydroxide or    potassium hydroxide in alcoholic medium such as, for example, in    methanol, or with hydrochloric acid or sulfuric acid.-   c) The possible alkylthio groups in the products described above, in    which the alkyl radical is optionally substituted with one or more    halogen atoms, especially fluorine, may, if desired, be converted    into the corresponding sulfoxide or sulfone functions under the    usual conditions known to those skilled in the art such as, for    example, with peracids such as, for example, peracetic acid or    meta-chloroperbenzoic acid, or with ozone, oxone or sodium periodate    in a solvent such as, for example, methylene chloride or dioxane at    room temperature.

The production of the sulfoxide function may be promoted with anequimolar mixture of the product containing an alkylthio group and thereagent such as, especially, a peracid.

The production of the sulfone function may be promoted with a mixture ofthe product containing an alkylthio group with an excess of the reagentsuch as, especially, a peracid.

-   d) The reaction for conversion of a ketone function into an oxime    may be performed under the usual conditions known to those skilled    in the art, such as, especially, a reaction in the presence of an    optionally O-substituted hydroxylamine in an alcohol such as, for    example, ethanol, at room temperature or with heating.-   e) The possible free or esterified carboxyl functions of the    products described above may be, if desired, reduced to an alcohol    function by the methods known to those skilled in the art: the    possible esterified carboxyl functions may be, if desired, reduced    to an alcohol function by the methods known to those skilled in the    art and especially with lithium aluminum hydride in a solvent such    as, for example, tetrahydrofuran or dioxane or ethyl ether. The    possible free carboxyl functions of the products described above may    be, if desired, reduced to an alcohol function especially with boron    hydride.-   f) The possible alkoxy functions such as, especially, methoxy, in    the products described above, may be, if desired, converted into a    hydroxyl function under the usual conditions known to those skilled    in the art, for example with boron tribromide in a solvent such as,    for example, methylene chloride, with pyridine hydrobromide or    hydrochloride or with hydrobromic acid or hydrochloric acid in water    or trifluoroacetic acid at reflux.-   g) The possible alcohol functions of the products described above    may be, if desired, converted into an aldehyde or acid function by    oxidation under the usual conditions known to those skilled in the    art, such as, for example, by the action of manganese oxide to    obtain the aldehydes, or of Jones' reagent to access the acids.-   h) The possible nitrile functions of the products described above    may be, if desired, converted into tetrazolyl under the usual    conditions known to those skilled in the art, such as, for example,    by cycloaddition of a metal azide such as, for example, sodium azide    or a trialkyltin azide on the nitrile function, as indicated in the    method described in the article referenced as follows:-   J. Organometallic Chemistry., 33, 337 (1971) KOZIMA S. et al.

It may be noted that the reaction for conversion of a carbamate intourea and especially of a sulfonylcarbamate into sulfonylurea may beperformed, for example, at the reflux point of a solvent such as, forexample, toluene, in the presence of the appropriate amine.

It is understood that the reactions described above may be performed asindicated or, where appropriate, according to other common methods knownto those skilled in the art.

-   i) The removal of protecting groups such as, for example, those    indicated above may be performed under the usual conditions known to    those skilled in the art, especially via an acid hydrolysis    performed with an acid such as hydrochloric acid, benzenesulfonic    acid or para-toluenesulfonic acid, formic acid or trifluoroacetic    acid, or via a catalytic hydrogenation.

The phthalimido group may be removed with hydrazine.

A list of various protecting groups that may be used will be found, forexample, in patent BF 2 499 995.

-   j) The products described above may, if desired, be subjected to    salification reactions, for example with a mineral or organic acid    or with a mineral or organic base according to the usual methods    known to those skilled in the art.-   k) The possible optically active forms of the products described    above may be prepared by resolving the racemic mixtures according to    the usual methods known to those skilled in the art.

The reaction of the products of formula (II) with the products offormula (III) is preferably performed in an organic solvent such astetrahydrofuran or dichloroethane, but ethyl ether or isopropyl ethermay also be used.

The process is optionally performed in the presence of a tertiary basesuch as triethylamine or pyridine or methylethylpyridine.

The possible reactive functions that are optionally protected in theproduct of formula (III), (IVa) or (IV″) are the hydroxyl or aminofunctions. Usual protecting groups are used to protect these functions.Examples include the following protecting groups for the amino radical:tert-butyl, tert-amyl, trichloroacetyl, chloroacetyl, benzhydryl,trityl, formyl, benzyloxycarbonyl.

Protecting groups for the hydroxyl radical that may be mentioned includeradicals such as formyl, chloroacetyl, tetrahydropyranyl, trimethylsilyland tert-butyldimethylsilyl.

It is clearly understood that the above list is not limiting and thatother protecting groups, which are known, for example, in peptidechemistry, may be used. A list of such protecting groups is found, forexample, in French patent 2 499 995, the content of which isincorporated herein by reference.

The possible reactions for removal of the protecting groups areperformed as indicated in said patent 2 499 995. The preferred method ofremoval is acid hydrolysis with acids chosen from hydrochloric acid,benzenesulfonic acid or para-toluenesulfonic acid, formic acid ortrifluoroacetic acid. Hydrochloric acid is preferred.

The possible reaction for hydrolysis of the >C═NH group to a ketonegroup is also preferably performed using an acid such as aqueoushydrochloric acid, for example at reflux.

The action on the products of formula (IV), (IVa) or (IV′) of thereagent of formula Hal-A2′-B2′-Y2′ is performed in the presence of astrong base such as sodium hydride or potassium hydride. The process maybe performed by phase-transfer reaction in the presence of quaternaryammonium salts such as tert-butylammonium.

An example of removal of the tert-butyldimethylsilyl group usinghydrochloric acid is given below in the examples.

The possible esterification of a free OH radical is performed understandard conditions. An acid or a functional derivative, for example ananhydride such as acetic anhydride in the presence of a base such aspyridine, may be used, for example.

The possible esterification or salification of a COOH group is performedunder the standard conditions known to those skilled in the art.

The possible amidation of a COOH radical is performed under standardconditions. A primary or secondary amine may be used on a functionalderivative of the acid, for example a symmetrical or mixed anhydride.

A subject of the present invention is also a process for preparing theproducts of formula (I″):

in which Y′, Y1′, Al, R, R1, R2′ and R3′ have the meanings given above,characterized in that a product of formula (V):

in which Al, Y1′ and Y2′ have the above meanings and Hal is a halogenatom, is reacted with a product of formula (VI):

in which R, R1, R2′, R3′ and X have the above meanings, the reactionbeing performed in the presence of a catalyst and optionally a solvent.

As regards the products of formula (V), the term “Hal” preferablydenotes a chlorine atom, but may also denote a bromine or iodine atom.

A subject of the invention is, more specifically, a process as definedabove in which the catalyst is a metal in native or oxidized form or abase.

The catalyst used may be a metal in native form, in metal oxide form orin the form of metal salts. The catalyst may also be a base. When thecatalyst used is a metal, this metal may be copper or nickel.

The metal salts may be a chloride or an acetate.

It may be noted that when A1 is single bond, a catalyst may be used.When A1 is alkyl, it is then an alkylation, which may be performedespecially in the presence of a reagent such as a base.

When the catalyst is a base, this base may be, for example, sodiumhydroxide or potassium hydroxide and, if desired, dimethyl sulfoxide maybe added to the reaction medium.

A subject of the invention is, more specifically, a process as definedabove in which the catalyst is chosen from cuprous oxide, cupric oxide,copper in native form and a base such as sodium hydroxide or potassiumhydroxide.

The copper in native form used as catalyst is preferably in the form ofpowder.

A subject of the invention is particularly a process as defined above inwhich the catalyst is cuprous oxide.

The solvent used is preferably chosen from high-boiling ethers such as,for example, phenyl oxide, diglyme, triglyme and dimethyl sulfoxide, butmay also be, for example, a high-boiling oil such as paraffin or liquidpetroleum jelly.

It may be noted that, especially when A1 is single bond, in the reactionof a product of formula (V) with a product of formula (VI) as definedabove, palladium or a salt thereof as described, for example, in thefollowing articles, or a copper salt with a ligand, for instance a1.2-diaminocyclohexane derivative, may also be used as catalyst:Buchwald S. L., J. AM. CHEM. SOC., 2002, 6043 and Buchwald S. L., J. AM.CHEM. SOC., 2001, 7727.

A subject of the invention is, more particularly, a process as definedabove, characterized in that the process is performed in the presence ofa solvent of ether type such as phenyl ether, diglyme, triglyme,dimethyl sulfoxide, toluene or dioxane.

A subject of the invention is, most particularly, a process as definedabove in which the solvent used is phenyl ether or triglyme.

The process for preparing the desired product, defined above, may beperformed under pressure or at atmospheric pressure, preferably atelevated temperature.

A subject of the invention is thus a process as defined above,characterized in that the reaction is performed at a temperature above100° C. and preferably above 150° C.

A subject of the invention is, more specifically, a process as definedabove, characterized in that the reaction is performed for more than 2hours.

A subject of the invention is, very specifically, a process as definedabove, characterized in that the reaction is performed in the presenceof cuprous oxide, in triglyme, at a temperature of greater than or equalto 200° C. and for more than 3 hours.

The products that are the subject of the present invention haveadvantageous pharmacological properties: it has been found that theyespecially have inhibitory properties on protein kinases.

Among these protein kinases, mention may be made especially of IGF1R.

FAK may also be mentioned. AKT may also be mentioned.

Tests given in the experimental section below illustrate the inhibitoryactivity of products of the present invention with respect to suchprotein kinases.

These properties thus make the compound of formula I of the presentinvention usable as medicinal products for treating malignant tumors.

The compound of formula I may also be used in the veterinary field.

A subject of the invention is thus, as medicinal products,pharmaceutically acceptable compound of formula I.

A subject of the invention is, particularly, the use as medicinalproducts of the products whose names are below:

-   (S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (S)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethane-sulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-4-methyl-3-quinol-4-ylmethyl-5-thioxo-1-(4-trifluoromethylsulfanylphenyl)imidazolidin-2-one    trifluoroacetate;-   (R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(4-hydroxybenzyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(4-hydroxybenzyl)-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   (R)-5-(1-hydroxyethyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-pyrid-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   (R)-1-(3-hydroxypyrid-4-ylmethyl)-5-methyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   4-quinol-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate;-   4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione    trifluoroacetate, said compound of formula I being in any possible    racemic, enantiomeric or diastereoisomeric isomer form, and also the    addition salts of said compound of formula I with pharmaceutically    acceptable mineral and organic acids or with pharmaceutically    acceptable mineral and organic bases.

A subject of the invention is particularly the use, as medicinalproducts, of the products whose names are given below:

-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}cyclopropanecarboxamide    trifluoroacetate;-   5,5-dimethyl-1-[2-(pyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione,    compound with trifluoroacetic acid;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}    isobutyramide, compound with trifluoroacetic acid;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide,    compound with trifluoroacetic acid;-   1-(2-aminopyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)-imidazolidine-2,4-dione    hydrochloride;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}pyridine-2-carboxamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-piperid-1-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-[4-(2-hydroxyethyl)piperazin-1-yl]propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-morpholin-4-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-pyrrolidin-1-ylpropionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-methylpiperazin-1-yl)propionamide    trifluoroacetate;-   1-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-phenylurea;-   1-[2-(6-ethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpyrid-2-ylamino)pyri-din-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(6-methylpyrid-2-ylamino)pyri-din-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imi-dazolidine-2,4-dione;-   1-[2-(4,6-dimethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(3,5-dichloropyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(pyrid-4-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(pyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)-imidazolidine-2,4-dione;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2-oxoazepan-1-yl)propionamide;-   3-(benzylmethylamino)-N-{4-[5,5-dimethyl-2,4-di-oxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   4,5-diacetoxy-6-acetoxymethyl-2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureidoacetic    acid;-   5,5-dimethyl-1-[2-(5-methylpyrid-2-ylamino)pyri-din-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3,5-dimethoxybenzamide    trifluoroacetate;-   5,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3-methylpiperid-1-yl)propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3,5-dimethylpiperid-1-yl)propionamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-methoxybenzamide    trifluoroacetate;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}pyrazine-2-carboxamide    trifluoroacetate;-   {4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thiophene-2-carboxamide    trifluoroacetate;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-4-methylbenzamide;    compound with trifluoroacetic acid;-   1-isoquinolin-5-yl-5,5-dimethyl-3-(4-trifluoro-methylsulfanylphenyl)imidazolidine-2,4-dione;-   3-(4-acetylpiperazin-1-yl)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   3-[4-(2-diethylaminoethyl)piperazin-1-yl]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2,6-dimethylmorpholin-4-yl)propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-pyrrolidin-1-ylpiperid-1-yl)propionamide;-   N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-(4-pyrrolidin-1-ylpiperid-1-yl)acetamide;-   5,5-dimethyl-1-[2-(4-methylpyrid-3-ylamino)pyri-din-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(6-morpholin-4-ylpyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2,6-dimethylpyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   methyl    5-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-ylamino}pyridine-2-carboxylate;-   1-[2-(2,6-dimethoxypyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(6-fluoropyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(6-methoxypyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione,    said compound of formula I being in any possible racemic,    enantiomeric or diastereoisomeric isomer form, and also the addition    salts of said compound of formula I with pharmaceutically acceptable    mineral and organic acids or with pharmaceutically acceptable    mineral and organic bases.

The products may be administered via the parenteral, oral, perlingual,rectal or topical route.

A subject of the invention is also pharmaceutical compositions,characterized in that they contain, as active principle, at least one ofthe medicinal compound of formula I.

These compositions may be in the form of injectable solutions orsuspensions, tablets, coated tablets, capsules, syrups, suppositories,creams, ointments and lotions. These pharmaceutical forms are preparedaccording to the usual methods. The active principle may be incorporatedinto excipients usually used in these compositions, such as aqueous ornonaqueous vehicles, talc, gum arabic, lactose, starch, magnesiumstearate, cocoa butter, fatty substances of animal or plant origin,paraffin derivatives, glycols, various wetting, dispersing oremulsifying agents, and preserving agents.

The usual dose, which varies according to the individual treated and thecomplaint under consideration, may be, for example, from 10 mg to 500 mgper day orally in man.

The present invention thus relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I for the preparation of medicinal products forinhibiting the activity of protein kinases and especially of a proteinkinase.

The present invention thus relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I in which the protein kinase is a protein tyrosinekinase.

The present invention thus relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I in which the protein kinase is chosen from thefollowing group: EGFR, Fak, FLK-1, FGFR1, FGFR2, FGFR3, FGFR4, FGFR5,flt-1, IGF-1R, KDR, PDGFR, tie2, VEGFR, AKT, Raf.

The present invention thus relates particularly to the use of compoundof formula I as defined above or of pharmaceutically acceptable salts ofsaid compound of formula I in which the protein kinase is IGF1R.

The present invention also relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I in which the protein kinase is FAK.

The present invention also relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I in which the protein kinase is AKT.

The present invention also relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I in which the protein kinase is in a cell culture,and also to this use in a mammal.

The present invention thus relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I for the preparation of a medicinal product forpreventing or treating a disease characterized by deregulation of theactivity of a protein kinase and especially such a disease in a mammal.

The present invention relates to the use of compound of formula I asdefined above or of pharmaceutically acceptable salts of said compoundof formula I for the preparation of a medicinal product for preventingor treating a disease belonging to the following group: disorders ofblood vessel proliferation, fibrotic disorders, disorders of mesangialcell proliferation, metabolic disorders, allergies, asthma, thrombosis,diseases of the nervous system, retinopathy, psoriasis, rheumatoidarthritis, diabetes, muscle degeneration, oncology diseases and cancer.

The present invention thus relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I for the preparation of a medicinal product fortreating oncology diseases.

The present invention relates particularly to the use of compound offormula I as defined above or of pharmaceutically acceptable salts ofsaid compound of formula I for the preparation of a medicinal productfor treating cancers.

Among these cancers, the present invention is most particularly ofinterest in the treatment of solid tumors and the treatment of cancersthat are resistant to cytotoxic agents.

Among these cancers, the present invention relates most particularly tothe treatment of breast cancer, stomach cancer, cancer of the colon,lung cancer, cancer of the ovaries, cancer of the uterus, brain cancer,cancer of the kidney, cancer of the larynx, cancer of the lymphaticsystem, cancer of the thyroid, cancer of the urogenital tract, cancer ofthe tract including the seminal vesicle and prostate, bone cancer,cancer of the pancreas and melanomas.

The present invention is even more particularly of interest in treatingbreast cancer, cancer of the colon and lung cancer.

The protein kinase IGF1-R (Insulin Growth Factor-1 Receptor) isparticularly indicated.

The protein kinase FAK is also indicated.

The protein kinase AKT is also indicated.

The present invention thus relates particularly to novel inhibitors ofthe IGF-1R receptor that may be used for oncology treatments.

The present invention also relates to novel FAK receptor inhibitors thatmay be used for oncology treatments.

The present invention also relates to novel AKT receptor inhibitors thatmay be used for oncology treatments.

Among the kinases for which a modulation of the activity is desired, FAK(Focal Adhesion Kinase) is also a preferred kinase.

The present invention also relates to the use of compound of formula Ias defined above or of pharmaceutically acceptable salts of saidcompound of formula I for the preparation of a medicinal product forcancer chemotherapy.

As medicinal products according to the present invention for cancerchemotherapy, the compound of formula I according to the presentinvention may be used alone or in combination with chemotherapy orradiotherapy or in combination with other therapeutic agents.

The present invention thus relates especially to the pharmaceuticalcompositions as defined above, also containing active principles ofother chemotherapy medicinal products for combating cancer.

Such therapeutic agents may be commonly used antitumor agents.

As examples of known inhibitors of protein kinases, mention may be madeespecially of butyrolactone, flavopiridol,2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine, olomucine, Glivecand Iressa.

The compound of formula I according to the present invention may thusalso be advantageously used in combination with antiproliferativeagents: as examples of such antiproliferative agents, but without,however, being limited to this list, mention may be made of aromataseinhibitors, antiestrogens, the topoisomerase I inhibitors, thetopoisomerase II inhibitors, microtubule-active agents, alkylatingagents, histone deacetylase inhibitors, farnesyl transferase inhibitors,COX-2 inhibitors, MMP inhibitors, mTOR inhibitors, antineoplasticantimetabolites, platinum compounds, compounds that reduce the activityof protein kinases and also anti-angiogenic compounds, gonadorelinagonists, antiandrogens, bengamides, biphosphonates and trastuzumab.

Examples that may thus be mentioned include anti-microtubule agents, forinstance taxoids, vinca alkaloids, alkylating agents such ascyclophosphamide, DNA-intercalating agents, for instance cis-platinum,agents that are interactive on topoisomerase, for instance camptothecinand derivatives, anthracyclines, for instance adriamycin,antimetabolites, for instance 5-fluorouracil and derivatives, and thelike.

The present invention thus relates to compound of formula I as proteinkinase inhibitors, said compound of formula I being in any possibleracemic, enantiomeric or diastereoisomeric isomer form, and also theaddition salts of said compound of formula I with pharmaceuticallyacceptable mineral and organic acids or with pharmaceutically acceptablemineral and organic bases, and also the prodrugs thereof.

The present invention relates particularly to compound of formula I asdefined above as IGF1R inhibitors.

The present invention also relates to compound of formula I as definedabove as FAK inhibitors.

The present invention also relates to compound of formula I as definedabove as AKT inhibitors.

The present invention relates more particularly to the products offormula (IA) as defined above as IGF1R inhibitors.

The compound of formula I according to the present invention may beprepared by application or adaptation of known methods and especially ofthe methods described in the literature such as, for example, thosedescribed by R. C. Larock in: Comprehensive Organic Transformations, VCHpublishers, 1989.

In the reactions described below, it may be necessary to protectreactive functional groups such as, for example, hydroxyl, amino, imino,thio or carboxyl groups, when these groups are desired in the finalproduct but when their participation is not desired in the reactions forsynthesizing the compound of formula I. Conventional protecting groupsmay be used in accordance with the usual standard practices, forinstance those described, for example, by T. W. Greene and P. G. M. Wutsin “Protective Groups in Organic Chemistry” John Wiley and Sons, 1991.

The products of formula (II) used at the start of the invention may beobtained by the action of phosgene when X is an oxygen atom, or ofthiophosgene when X is a sulfur atom, on the corresponding amine offormula (A), i.e., the aminophenyl derivative bearing the substituents Yand Y1′ as defined above.

A product of this type is also described in French patent 2 329 276.

The products of formula (III) or (III′) are known or may be preparedfrom the corresponding cyanohydrin according to the process described inthe publication: J. Am. Chem. Soc. (1953), 75, 4841.

The products of formula (III) may be obtained by the action of a productof formula Y2-B2-A2-Hal on 2-cyano-2-aminopropane under the conditionsstated above for the action of Y2-B2-A2-Hal on the products of formula(IV). An example of a preparation of this type is described in thereference:

-   -   Jilek et al. Collect. Czech. Chem. Comm. 54(8) 2248 (1989).

The products of formula (IV′) are described in French patent 2 329 276.

The starting materials of formulae (V) and (VI), on which a process thatis the subject of the invention is performed, to obtain the compound offormula I, are known and commercially available or may be preparedaccording to methods known to those skilled in the art.

The preparation of products of formula (VI) is described especially inthe following publications:

-   -   Zhur. Preklad. Khim. 28, 969-75 (1955) (CA 50, 4881a, 1956);    -   Tetrahedron 43, 1753 (1987);    -   J. Org. Chem. 52, 2407 (1987);    -   Zh. Org. Khim. 21, 2006 (1985);    -   J. Fluor. Chem. 17, 345 (1981)        or in:    -   German patent DRP 637 318 (1935);    -   European patent EP 0 130 875;    -   Japanese patent JP 81 121 524.

The products of formula (VI) that are hydantoin derivatives are widelyused and cited in the literature, for instance in the followingarticles:

-   -   J. Pharm. Pharmacol., 67, Vol. 19(4), p. 209-16 (1967);    -   Khim. Farm. Zh., 67, Vol. 1 (5) p. 51-2;    -   German patent 2 217 914;    -   European patent 0 091 596;    -   J. Chem. Soc. Perkin. Trans. 1, p. 219-21 (1974).

The compound of formula I of the present patent application as definedabove, for which p is 0 and which thus constitute hydantoin derivatives,may be synthesized according to the process indicated above andespecially according to the general scheme below which describes thissynthesis on a solid support. The protocol that follows this schemegives the operating conditions for such a synthesis of the compound offormula I of the present patent application on a solid support.

The experimental section below more particularly gives an illustrationof such a synthesis on a solid support according to the above protocolwith the preparation of Examples 1 to 56 of the present patentapplication.

Such a synthesis may be performed according to the general protocolbelow. Rink resin, protected with an Fmoc group, is deprotected with a20% solution of piperidine in DMF. The resulting amine resin is coupledwith an amino acid protected with an Fmoc group, in the presence ofdiisopropylaminecarbodiimide (DIC) and hydroxybenzotriazole (HOBt). Thesupported N-Fmoc amino acid is then deprotected with a 20% solution ofpiperidine in DMF. The free amine is reacted with an aldehyde dissolvedin a 50/50 mixture of THF and triethyl orthoformate (TEOF) to give aSchiff's base, which is reduced with sodium cyanoborohydride. Theresulting amine is coupled with an isocyanate or an isothiocyanate togive the corresponding urea or thiourea. When the isocyanate is notcommercially available, it may be prepared from the corresponding amineby reaction with ⅓ equivalent of triphosgene in the presence of 2equivalents of pyridine. The product is then cleaved with a 95%trifluoroacetic acid/water mixture. The urea thus released cyclizes togive the expected hydantoinine. In certain cases, the cleavage solutionmust be heated to 80° C. to obtain complete cyclization.

The compound of formula I of the present patent application as definedabove, for which p is 1 and which thus constitute dihydrouracilderivatives, may be synthesized according to the process indicated aboveand especially according to the general scheme below which describesthis synthesis on a solid support. The protocol that follows this schemegives the operating conditions for such a synthesis of the compound offormula I of the present patent application on a solid support.

The experimental section below more particularly gives an illustrationof such a synthesis on a solid support according to the above protocolwith the preparation of Example 5 of the present patent application.

For the synthesis of the dihydrouracils on a solid support, the protocolthat follows may be used.

Wang polystyrene resin (1.7 mmol/g) is used, for example, which resin istreated with a mixture of β-amino acid, 2,6-dichlorobenzoyl chloride andpyridine in DMF. After washing, the resin is treated with a 10% solutionof piperidine in DMF. The resulting free amine is reacted with analdehyde in a mixture of THF/trimethyl orthoformate (TMOF). Theresulting Schiff's base is reduced with sodium cyanoborohydride in amixture of methanol, THF and acetic acid. The secondary amine obtainedis acylated with phosgene and the resulting carbamoyl chloride istreated with a primary amine to give the corresponding urea. Cyclizationto the dihydrouracil and cleavage of the final product are performed bytreating with a strong base such as diazabicycloundecene (DBU).

The compound of formula I of the present patent application may thus besynthesized on a solid support as described above or in liquid phaseaccording to the process indicated below: the experimental section ofthe present patent application gives an illustration of such aliquid-phase synthesis with the preparation of Examples 57 to 62.

For this liquid-phase synthetic process, two routes A and B may beperformed, each involving two steps.

Route A:

-   step a: the alkylation of the amino ester may be performed by    reductive amination with an aromatic or heterocyclic aldehyde    according to the general process described in Advanced Organic    Reaction, March, third edition, page 798-800. In particular, the    formation of the Schiff's base (intermediate) may be performed using    an amino ester optionally in salt form, an aldehyde and optionally a    dehydrating agent (for example magnesium sulfate) in a solvent, for    instance dichloromethane or dichloroethane, at a temperature of    between 0° C. and the reflux point of the solvent. The imine formed    may be isolated. The imine formed is reduced with a metal hydride,    for instance sodium borohydride, in a solvent, for instance an    alcohol (for example ethanol or methanol), at a temperature of    between 0° C. and the reflux point of the solvent.-   step b: the amino ester obtained is coupled with an isocyanate in a    solvent, for instance THF or dichloromethane, with or without the    presence of a base (for example triethylamine) or an acid (for    example trifluoroacetic acid), at a temperature of between 0° C. and    the reflux point of the solvent. When the isocyanates are not    commercially available, they are prepared from the corresponding    amines and triphosgene or diphosgene or phosgene in the presence of    a base (for example pyridine or triethylamine) according to the    general procedure described in Advanced Organic Reaction, March,    third edition, page 370.    Route B:-   step a: the formation of the isocyanate may be performed by coupling    an aromatic or heterocyclic amine with diphosgene in the presence of    activated plant charcoal, in a solvent, for instance toluene, at a    temperature of between −40° C. and the reflux point of the solvent.    The isocyanate formed is not isolated, and may react with the amino    ester or its salt in the same solvent in the presence of a base, for    instance triethylamine, at a temperature of between 0° C. and the    reflux point of the solvent, to give the    3-arylimidazolidine-2,4-dione derivative.-   step b: the coupling of this derivative with an alkyl halide is    performed in the presence of a base, for instance potassium    tert-butoxide or sodium hydride, in a solvent, for instance THF or    DMF, at a temperature of between 0° C. and the reflux point of the    solvent.

The compound of formula I of the present patent application whichconstitute Examples 201 to 207 of the present patent application wereprepared as indicated below in the experimental section and as indicatedin the following schemes: in these schemes, Example I is Example 201,Example II is Example 202, Example III is Example 203, Example IV isExample 204, Example V is Example 205, Example VI is Example 206 andExample VII is Example 207.

EXAMPLES I and II

EXAMPLES III and IV

EXAMPLES V, VI and VII

The synthesis of the compound of formula I of the present patentapplication which constitute the products of Examples 208 to 243 wereperformed using route B. The alkyl halide may be prepared from thecorresponding carboxylic acids.

The ethyl carboxylates were prepared by esterification of the carboxylicacids in ethanol in the presence of sulfuric acid, adopting theconditions described in Synthesis 2000, 1138.

The reduction of the ethyl carboxylates in alcohol was performed inethanol in the presence of sodium borohydride, adopting the conditionsdescribed in Synthesis 2000, 1665.

The conversion of the alcohols thus obtained into alkyl halides wasperformed using dibromotriphenylphosphorane as halogenating agent,adopting the conditions described in J. Heterocyclic Chem., 30, 631(1993).

The alkyl halides may also be prepared by free-radical bromination ofthe corresponding methylenes in the presence of N-bromosuccinimide andbenzoyl peroxide in carbon tetrachloride, adopting the conditionsdescribed in J. Heterocyclic Chem., 30, 631 (1993).

Thus, we functionalized the pyridine nucleus in position -2 with abromine or fluorine atom or with a nitrile group.

The latter compound will also allow us to prepare various carbonylcompounds.

Acidic hydrolysis of the nitrile in the presence of sulfuric acid,adopting the conditions described in J. Med. Chem. 1991, 34, 281-290,led to the carboxamide in dimeric form. Hydrolysis of the nitrile undermilder conditions allowed the expected carboxamide to be obtained.

Acidic hydrolysis of the nitrile in the presence of 5N hydrochloricacid, adopting the conditions described in J. Heterocyclic Chem., 30,631 (1993), gave the corresponding carboxylic acid.

The amide could be obtained from the carboxylic acid using1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as couplingagent in dichloromethane, adopting the conditions described in J. Am.Chem. Soc., 95, 875, (1973). Various amino analogs were obtained bynucleophilic substitution of the chloro intermediate with amines underirradiation in a microwave oven, inspired by the conditions described inTetrahedron 2002, 58, 1125.

X NR1R2 NR1R2 NR1R2 O

S

The amino analog was obtained by deprotection of thep-methoxybenzylamine group in the presence of trifluoroacetic acid,inspired by the conditions described in J. Chem. Soc., Perkin Trans. 1,2002, 428-433.

This amino derivative allowed access to other chemical functions, forinstance the amide function, the carbamate function or the sulfonamidefunction.

The acetamido derivative was obtained by acylation of the aminoderivative in the presence of acetic anhydride, inspired by theconditions described in Tetrahedron Lett. 2002, 43, 3121. We alsoprepared the methyl and tert-butyl carbamates inspired by the conditionsdescribed in J. Heterocyclic Chem., 22, 313 (1985) and in J. Org. Chem.2002, 67, 4965. The amino derivative was also sulfonylated with mesylchloride, inspired by the conditions described in J. Med. Chem., 1985,28, 824.

The above conditions were also used for the synthesis of the compoundscontaining a disubstituted phenyl group.

The hydantoin containing a pyridine nucleus disubstituted in position−2.6 with a bromine atom was prepared using the above conditions,starting with 2,6-dibromo-4-(hydroxymethyl)pyridine described inSynthesis 2000, 1665.

The products may be purified as follows:

Purification by LC/MS

The products may be purified by LC/MS using a Waters FractionLynx systemcomposed of a Waters model 600 gradient pump, a Waters model 515regeneration pump, a Waters Reagent Manager dilution pump, a Watersmodel 2700 autoinjector, two Rheodyne LabPro model valves, a Watersmodel 996 diode array detector, a Waters model ZMD mass spectrometer anda Gilson model 204 fraction collector. The system was controlled by theWaters FractionLynx software. The separation was performed alternatelyon two Waters Symmetry columns (C₁₈, 5 μM, 19×50 mm, catalog reference186000210), one column undergoing regeneration with a 95/5 (v/v)water/acetonitrile mixture containing 0.07% (v/v) trifluoroacetic acid,while the other column was performing separation. The columns wereeluted using a linear gradient of from 5% to 95% of acetonitrilecontaining 0.07% (v/v) of trifluoroacetic acid in water containing 0.07%(v/v) trifluoroacetic acid, at a flow rate of 10 ml minute. At theseparation column outlet, one-thousandth of the effluent is separated byan LC Packing Accurate, diluted with methyl alcohol, at a flow rate of0.5 ml/minute, and sent to the detectors, in a proportion of 75% to thediode array detector and the remaining 25% to the mass spectrometer. Therest of the effluent (999/1000) is sent to the fraction collector, wherethe flow is discarded as long as the mass of the expected product hasnot been detected by the FractionLynx software. The molecular formulaeof the expected products are supplied to the FractionLynx software,which initiates the collection of the product when the mass signaldetected corresponds to the ion [M+H]⁺ and/or to [M+Na]⁺. In certaincases, depending on the analytical LC/MS results, when an intense ioncorresponding to [M 2H]⁺+ was detected, the value corresponding to halfthe calculated molecular mass (MW/2) is also supplied to theFractionLynx software. Under these conditions, collection is alsoinitiated when the mass signal of the ion [M2H]⁺⁺ and/or [M+Na⁺H]⁺⁺ isdetected. The products were collected in tared glass tubes. Aftercollection, the solvents were evaporated off, in a Savant AES 2000 orGenevac HT8 centrifuge evaporator and the product masses were determinedby weighing the tubes after evaporating off the solvents.

The LC/MS analyses were performed on a Micromass LCT model machineconnected to an HP 1100 machine. The abundance of the products wasmeasured using an HP G1315A diode array detector over a wavelength rangefrom 200-600 nm and a Sedex 65 light scattering detector. Theacquisition of the mass spectra was performed over a range from 180 to800. The data were analyzed using the Micromass MassLynx software. Theseparation was performed on a Hypersil BDS C18, 3 μm column (50×4.6 mm),eluting with a linear gradient of from 5% to 90% of acetonitrilecontaining 0.05% (v/v) trifluoroacetic acid (TFA) in water containing0.05% (v/v) TFA over 3.5 minutes at a flow rate of 1 ml/minute. Thetotal analysis time, including the column reequilibration time, is 7minutes.

The products of Examples 244 to 255 of the present invention wereprepared as indicated in the experimental section and according to thegeneral synthetic route of the scheme below:

The products of Examples 256 to 263 of the present invention wereprepared according to reaction Schemes 1 and 2 indicated below, in whichthe FIGS. 1 to 8 correspond, respectively, to Examples 256 to 263: theproducts of Examples 256 to 261 (i.e. products 1 to 6) were preparedaccording to Scheme 1 and the two thiohydantoin compounds of Examples262 and 263 (i.e. products 7 and 8) were prepared according to Scheme 2.

The nitro compound is prepared by nitration of methyl2-trifluoromethoxybenzoate by nitration (fuming nitric acid) bycontrolling the temperature.

According to the conditions described in patent PCT Int. Appl. (2000),564: WO 0069810.

The corresponding amine is prepared by reduction of the nitro functionin the presence of SnCl₂ in ethanol, according to the same patent.

The isocyanate is prepared by reacting diphosgene dissolved in tolueneat −20° C. under the usual known conditions. The isocyanate is reactedwith the quinoline derivative prepared according to the known methods,in order to prepare the desired hydantoin.

The acid is obtained by saponification using 2N sodium hydroxide in THFat 60° C.

The amide is prepared by coupling the desired amine using EDCI ascoupling agent (standard coupling conditions).

The alcohol is obtained by reducing the ester in THF in the presence ofLiAlH₄.

The halo derivatives R═Cl and R═Br are prepared from the commercialanilines according to the same synthetic scheme.

The examples whose preparation follows illustrate the present inventionwithout, however, limiting it.

EXAMPLE 1 Preparation of(S)-5-methyl-1-quinolin-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

2 g (1.02 mmol) of Polystyrene AM RAM (Rink resin) (0.51 mmol/g) aresuspended in 20 ml of DMF in a 50 ml syringe fitted with a sinter. Afteragitation for 10 minutes, the DMF is filtered and replaced with 10 ml ofa 20% solution of piperidine in DMF. After agitation for one hour atroom temperature, the solution is filtered and the resin washedsuccessively with 3×10 ml of DMF, 2×10 ml of methanol and 3×10 ml ofDMF. A solution of 0.94 g of Fmoc-Ala(OH) (3 mmol), 0.41 g of HOBt (3mmol) and 0.48 ml of DIC (3 mmol) in 10 ml of DMF is added to the resin.The syringe is agitated overnight at room temperature and the resin isthen washed successively with 5×10 ml of DMF, 3×10 ml of MeOH and 5×10ml of DCM. Next, 10 ml of a 20% solution of piperidine in DMF areintroduced into the syringe. After agitation for 1 hour, the solution isfiltered and the resin washed with 5×10 ml of DMF, 2×10 ml of MeOH, 3×10ml of DCM and 3×10 ml of THF. Next, a solution of 0.79 g ofquinoline-4-carboxaldehyde (5.1 mmol) in 10 ml of a 50/50 THF/TEOFmixture is added to the resin. After agitation overnight at roomtemperature, the solution is filtered and the resin washed with 10×10 mlof THF. 0.63 g of sodium cyanoborohydride in a mixture of 1.5 ml ofMeOH, 3.5 ml of dichloroethane and 0.1 ml of acetic acid is then addedto the resin. The resin is agitated overnight and then, afterfiltration, washed with 10×10 ml of DCM, 3×10 ml of MeOH and 5×10 ml ofDCM.

In parallel, a solution of 0.563 g of4-(trifluoromethanesulfonyl)aniline (2.5 mmol) is treated with 0.25 g oftriphosgene (0.83 mmol), followed by 0.23 ml of pyridine (2.5 mmol) at0° C. under nitrogen. After the temperature has warmed gradually to roomtemperature, the reaction is stirred for 2 hours and a further 0.23 mlof pyridine in 1 ml of DMF is added to the mixture. The solutionobtained is transferred into the syringe, which is agitated for 2 hours.The solution is then filtered and the resin washed with 5×10 ml of DCM,3×10 ml of MeOH and 5×10 ml of DCM. Finally, the resin is treated with 5ml of a 95% solution of trifluoroacetic acid in water. The mixture isagitated for 2 hours and then filtered. The resin is washed with 2 ml ofMeOH, followed by 2 ml of DCM. The combined filtrates are evaporatedunder vacuum. 280 mg of crude product are thus obtained. Afterpurification by preparative LC-MS, 240 mg (overall yield=41%) ofexpected product are isolated in the form of a white solid.

EIMS ([M+H]+: 464

Retention time (RT)=3.12 min (YMC basic S5 column; 2-85% ACN/H₂Ogradient over 7 min)

1H NMR (300 MHz) (CDCl₃): 1.59 (d, 3H); 4.11(t, 1H); 5.01 and 5.55(AB,2H); 7.70 (d,

1H); 7.89 (m, 1H); 7.99 (m, 3H); 8.15 (m, 2H); 8.30 (d, 1H), 8.50 (d,1H); 9.22 (d, 1H).

EXAMPLE 2 Preparation of(S)-4-methyl-3-quinol-4-ylmethyl-5-thioxo-1-(4-trifluoromethanesulfonylphenyl)imidazolidin-2-onetrifluoroacetate

Resin 3, 0.036 mmol, prepared according to Example 1, is used for thepreparation of the compound.

33 mg of thiocarbonyldiimidazole (0.18 mmol) are added to a solution of41 mg of 4-(trifluoromethanesulfonyl)aniline (0.18 mmol) in 3 ml of DCM.The reaction mixture is stirred for 2 hours at room temperature and thenadded directly to the resin. After stirring for 2 hours, the solution isfiltered and the resin is then washed with 5×2 ml of DCM, 3×5 ml of MeOHand 5×2 ml of DCM.

Finally, 2 ml of a 95% solution of TFA in water are added to the resin.After stirring for 2 hours, the mixture is filtered and the resin washedwith 1 ml of MeOH and 1 ml of DCM. The combined filtrates are heated at60° C. for 2 hours and then concentrated under vacuum. Afterpurification by preparative LC-MS, 1.8 mg of expected product areisolated.

EIMS [(M+H]⁺): 480

RT=4.72 min (YMC basic S5 column; 2-85% ACN/H₂O gradient over 7 min)

EXAMPLE 3 Preparation of(S)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.025 mmol of resin, 0.075 mmol ofN-Fmoc-L-Ala(OH), 0.125 mmol of 4-pyridinecarboxaldehyde and 0.0625 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 5.6 mg of expected product areobtained.

EIMS ([M+H]+): 414

RT=2.72 min

EXAMPLE 4 Preparation of(S)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.025 mmol of resin, 0.075 mmol ofN-Fmoc-L-Ala(OH), 0.125 mmol of 4-pyridinecarboxaldehyde and 0.0625 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 1.3 mg of expected product areobtained.

EIMS ([M+H]+): 382

RT=2.83 min

EXAMPLE 5 Preparation of(S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.025 mmol of resin, 0.075 mmol ofN-Fmoc-L-Ala(OH), 0.125 mmol of 4-quinolinecarboxaldehyde and 0.0625mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 0.6 mg of expectedproduct is obtained.

EIMS ([M+H]+): 432

RT=3.14 min

EXAMPLE 6 Preparation of1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 4 mmol of resin, 12 mmol ofN-Fmoc-Gly(OH), 20 mmol of 4-quinolinecarboxaldehyde, and 10 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 1 g of expected product isobtained.

EIMS ([M+H]+): 450

RT=3.20 min

EXAMPLE 7 Preparation of5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.25 mmol of resin, 0.75 mmol ofFmoc-AIB-(OH), 1.25 mmol of 4-quinolinecarboxaldehyde and 0.625 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 22 mg of expected product areobtained.

EIMS ([M+H]+): 478

RT=4.26 min

EXAMPLE 8 Preparation of(R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 4-quinolinecarboxaldehyde and 0.10 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 10 mg of expected product areobtained.

EIMS ([M+H]+): 464

RT=4.36 min

EXAMPLE 9 Preparation of(R)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 4-quinolinecarboxaldehyde and 0.10 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 11 mg of expected product areobtained.

EIMS ([M+H]+): 432

RT=4.50 min

EXAMPLE 10 Preparation of(R)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.28 mmol of resin, 0.84 mmol ofN-Fmoc-D-Ala(OH), 1.4 mmol of 4-pyridinecarboxaldehyde and 0.70 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 105 mg of expected product areobtained.

EIMS ([M+H]+): 414

RT=2.40 min

EXAMPLE 11 Preparation of(R)-5-methyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.28 mmol of resin, 0.84 mmol ofN-Fmoc-D-Ala(OH), 1.4 mmol of 4-pyridinecarboxaldehyde and 0.70 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 91 mg of expected product areobtained.

EIMS ([M+H]+): 382

RT=2.52 min

EXAMPLE 12 Preparation of(S)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-L-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde and0.10 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 17 mg of expectedproduct are obtained.

EIMS ([M+H]+): 396

RT=4.20 min

EXAMPLE 13 Preparation of(S)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-L-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde, and0.10 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 16 mg of expectedproduct are obtained.

EIMS ([M+H]+): 428

RT=4.07 min

EXAMPLE 14 Preparation of(S)-4-methyl-3-pyrid-4-ylmethyl-5-thioxo-1-(4-trifluoromethylsulfanylphenyl)imidazolidin-2-onetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-L-Ala(OH), 0.20 mmol of 4-pyridinecarboxaldehyde and 0.10 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 2. Afterpurification by preparative LC-MS, 1.7 mg of expected product areobtained.

EIMS ([M+H]+): 398

RT=4.51 min

EXAMPLE 15 Preparation of(S)-4-methyl-3-pyrid-4-ylmethyl-5-thioxo-1-(4-trifluoromethanesulfonylphenyl)imidazolidin-2-onetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-L-Ala(OH), 0.20 mmol of 4-pyridinecarboxaldehyde and 0.10 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 2.After purification by preparative LC-MS, 2.2 mg of expected product areobtained.

EIMS ([M+H]+): 430

RT=4.34 min

EXAMPLE 16 Preparation of(R)-4-methyl-3-(3-methylpyrid-4-ylmethyl)-5-thioxo-1-(4-trifluoromethylsulfanylphenyl)imidazolidin-2-onetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde and0.10 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 2. After purification by preparative LC-MS, 1.9 mg of expectedproduct are obtained.

EIMS ([M+H]+): 412

RT=4.60 min

EXAMPLE 17 Preparation of(R)-4-methyl-3-(3-methylpyrid-4-ylmethyl)-5-thioxo-1-(4-trifluoromethylsulfonylphenyl)imidazolidin-2-onetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde and0.10 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 2. After purification by preparative LC-MS, 4.5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 444

RT=4.41 min

EXAMPLE 18 Preparation of(R)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde and0.10 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 14 mg of expectedproduct are obtained.

EIMS ([M+H]+): 396

RT=4.22 min

EXAMPLE 19 Preparation of(R)-5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxaldehyde and0.10 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 6.3 mg of expectedproduct are obtained.

EIMS ([M+H]+): 428

RT=4.10 min

EXAMPLE 20 Preparation of(R)-4-methyl-3-quinol-4-ylmethyl-5-thioxo-1-(4-trifluoromethylsulfanylphenyl)imidazolidin-2-onetrifluoroacetate

The compound is prepared from 0.04 mmol of resin, 0.12 mmol ofN-Fmoc-D-Ala(OH), 0.20 mmol of 4-qinolinecarboxaldehyde and 0.10 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 2. Afterpurification by preparative LC-MS, 0.4 mg of expected product isobtained.

EIMS ([M+H]+): 448

RT=4.89 min

EXAMPLE 21 Preparation of(R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Val(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 0.3 mg of expected product isobtained.

RT=4.01 min

EIMS ([M+H]+): 460

EXAMPLE 22 Preparation of(R)-5-isopropyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Val(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 1 mg of expected product isobtained.

EIMS ([M+H]+): 492

RT=3.91 min

EXAMPLE 23 Preparation of(R)-5-Benzyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Phe(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 8.9 mg of expected product areobtained.

EIMS ([M+H]+): 508

RT=4.11 min

EXAMPLE 24 Preparation of(R)-5-Benzyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Phe(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 5.9 mg of expected product areobtained.

EIMS ([M+H]+): 540

RT=4.01 min

EXAMPLE 25 Preparation of(R)-5-Benzyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Phe(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 11.1 mg of expected product areobtained.

EIMS ([M+H]+): 490

RT=3.76 min

EXAMPLE 26 Preparation of(R)-5-isobutyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Leu(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 5.9 mg of expected product areobtained.

RT=4.02 min

EIMS ([M+H]+): 506

EXAMPLE 27 Preparation of(R)-5-(4-hydroxybenzyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Tyr(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 5.1 mg of expected product areobtained.

EIMS ([M+H]+): 524

RT=3.75 min

EXAMPLE 28 Preparation of(R)-5-(4-hydroxybenzyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Tyr(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 1.8 mg of expected product areobtained.

EIMS ([M+H]+): 556

RT=3.66 min

EXAMPLE 29 Preparation of(R)-5-(4-hydroxybenzyl)-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Tyr(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 0.7 mg of expected product isobtained.

EIMS ([M+H]+): 506

RT=3.48 min

EXAMPLE 30 Preparation of(R)-5-(1-hydroxyethyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Thr(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanethio)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 4.2 mg of expected product areobtained.

EIMS ([M+H]+): 462

RT=3.52 min

EXAMPLE 31 Preparation of(R)-5-(1-hydroxyethyl)-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Thr(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmolof 4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 3.4 mg of expected product areobtained.

EIMS ([M+H]+): 494

RT=3.43 min

EXAMPLE 32 Preparation of4-quinol-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 7.5 mg of expected product areobtained.

EIMS ([M+H]+): 444

RT=3.68 min

EXAMPLE 33 Preparation of4-quinol-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 3.8 mg of expected product areobtained.

EIMS ([M+H]+): 476

RT=3.60 min

EXAMPLE 34 Preparation of4-pyrid-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and 0.125 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 1.7 mg of expected product areobtained.

EIMS ([M+H]+): 394

RT=3.43 min

EXAMPLE 35 Preparation of4-pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-pyridinecarboxaldehyde, and 0.125 mmol of4-(trifluoromethanesulfonyl)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 1.4 mg of expected product areobtained.

EIMS ([M+H]+): 426

RT=3.35 min

EXAMPLE 36 Preparation of(R)-5-benzo[b]thiophen-3-ylmethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-benzothienylAla(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 596

RT=4.12 min

EXAMPLE 37 Preparation of(R)-5-benzo[b]thiophen-3-ylmethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-benzothienylAla(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 1.4 mg of expectedproduct are obtained.

EIMS ([M+H]+): 514

RT=3.35 min

EXAMPLE 38 Preparation of(R)-5-benzo[b]thiophen-3-ylmethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-benzothienylAla(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 8.5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 546

RT=3.90 min

EXAMPLE 39 Preparation of(S)-5-pyrid-2-ylmethyl-1-quinol-4-ylmethyl-3-(4-trifluoro-methylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-2-pyridine-Ala(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 7.5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 509

RT=3.47 min

EXAMPLE 40 Preparation of(S)-5-pyrid-2-ylmethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-2-pyridine-Ala(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 1.6 mg of expectedproduct are obtained.

EIMS ([M+H]+): 541

RT=3.41 min

EXAMPLE 41 Preparation of(R)-1-(3-hydroxypyrid-4-ylmethyl)-5-methyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofN-Fmoc-D-Ala(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 8.3 mg of expectedproduct are obtained.

EIMS ([M+H]+): 398

RT=4.26 min

EXAMPLE 42 Preparation of5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmol of4-(trifluoromethoxy) aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 5.5 mg of expected product areobtained.

EIMS ([M+H]+): 430

RT=4.33 min

EXAMPLE 43 Preparation of5,5-dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 4-quinolinecarboxaldehyde, and 0.125 mmol of4-(trifluoromethanethio)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 9.4 mg of expected product areobtained.

EIMS ([M+H]+): 446

RT=4.58 min

EXAMPLE 44 Preparation of5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethoxy)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 5.5 mg of expected product areobtained.

EIMS ([M+H]+): 394

RT=4.06 min

EXAMPLE 45 Preparation of5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 13.1 mg of expectedproduct are obtained.

EIMS ([M+H]+): 410

RT=4.30 min

EXAMPLE 46 Preparation of5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 9.6 mg of expectedproduct are obtained.

EIMS ([M+H]+): 442

RT=4.18 min

EXAMPLE 47 Preparation of1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethoxy)aniline, in the same way as in Example 1.After purification by preparative LC-MS, 6.9 mg of expected product areobtained.

EIMS ([M+H]+): 394

RT=4.15 min

EXAMPLE 48 Preparation of1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 9.7 mg of expectedproduct are obtained.

EIMS ([M+H]+): 412

RT=4.39 min

EXAMPLE 49 Preparation of1-(3-hydroxypyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 15.2 mg of expectedproduct are obtained.

EIMS ([M+H]+): 444

RT=4.30 min

EXAMPLE 50 Preparation of4-quinol-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-quinolinecarboxaldehyde and 0.125 mmol of4-(trifluoromethoxy)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 4.1 mg of expected product areobtained.

EIMS ([M+H]+): 428

RT=4.24 min

EXAMPLE 51 Preparation of4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 4-pyridinecarboxaldehyde and 0.125 mmol of4-(trifluoromethoxy)aniline, in the same way as in Example 1. Afterpurification by preparative LC-MS, 3 mg of expected product areobtained.

EIMS ([M+H]+): 392

RT=3.95 min

EXAMPLE 52 Preparation of4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 408

RT=4.24 min

EXAMPLE 53 Preparation of4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxaldehyde and 0.125mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 1.9 mg of expectedproduct are obtained.

EIMS ([M+H]+): 440

RT=4.11 min

EXAMPLE 54 Preparation of4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethoxy)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 5.5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 394

RT=4.04 min

EXAMPLE 55 Preparation of4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanethio)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 0.7 mg of expectedproduct is obtained.

EIMS ([M+H]+): 410

RT=4.34 min

EXAMPLE 56 Preparation of4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dionetrifluoroacetate

The compound is prepared from 0.05 mmol of resin, 0.15 mmol ofFmoc-ACPC—(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxaldehyde and0.125 mmol of 4-(trifluoromethanesulfonyl)aniline, in the same way as inExample 1. After purification by preparative LC-MS, 2.5 mg of expectedproduct are obtained.

EIMS ([M+H]+): 442

RT=4.17 min

EXAMPLE 57 Preparation of5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)dihydropyrimidine-2,4-dione

588 mg (1 mmol) of Wang polystyrene resin (1.7 mmol/g) are washed with2×5 ml of DMF, 1×5 ml of DCM and then treated with a solution of 0.49 gof N-Fmoc-3-amino-2-(R,S)-methylpropionic acid (1.5 mmol), 0.24 g ofpyridine (3 mmol) in 5 ml of DMF, immediately followed by 0.31 g of2,6-dichlorobenzoyl chloride (dropwise addition to control theexothermicity). The reaction mixture is stirred overnight at roomtemperature. The mixture is filtered and the resin is then washed with1×5 ml of DMF, 1×5 ml of DCM and 2×5 ml of DMF and then treated with 5ml of a 10% solution of piperidine in DMF. The resin is then washed with2×5 ml of DMF, 1×5 ml of DCM, 1×5 ml of DMF, 1×5 ml of DMF, 4×5 ml ofDCM, 4×5 ml of MeOH and dried under vacuum. 0.94 g of4-quinolinecarboxaldehyde (6 mol) in 16 ml of a 50/50 mixture ofTHF/TMOF is added to the resin, which is stirred overnight. The resin isthen washed 3 times with 5 ml of the same THF/TMOF mixture and thentreated with 12 ml of a 1 M solution of sodium cyanoborohydride in THF(12 mmol) in the presence of 1.2 ml of MeOH and 0.12 ml of acetic acid.After stirring overnight at room temperature, the resin is washed with1×5 ml of THF, 4×5 ml of a 30% solution of acetic acid in DMF, 1×5 ml ofMeOH, 1×5 ml of THF, 1×5 ml of DMF, 1×5 ml of THF, 1×5 ml of MeOH anddried under vacuum.

In parallel, 0.121 g of triphosgene (0.41 mmol) in 1 ml of DCM is addeddropwise to a solution of 0.281 g of 4-(trifluoromethanesulfonyl)aniline(1.25 mmol) and 0.1 g of pyridine (1.25 mmol) in 2 ml of DCM. Afterstirring for 15 minutes at room temperature, the same amount of pyridineis added, followed by the resin previously prepared. The mixture isstirred overnight and then filtered. The resin is washed with 1×5 ml ofMeOH, 1×5 ml of THF, 1×5 ml of MeOH, 1×5 ml of DMF, 1×5 ml of THF, 1×5ml of MeOH and 3×5 ml of THF and dried under vacuum. The resin is thentreated with 154 mg of DBU (1 mmol) in 5 ml of DCM and stirredovernight. Finally, the dihydrouracil is obtained by treating the resinwith 5 ml of 2% solution of acetic acid in THF. After purification bypreparative HPLC, 90 mg of expected product are isolated.

EIMS ([M+H]+): 477

RT=1.83 min (20-100% ACN/H₂O gradient over 5 minutes)

EXAMPLE 58(S)-5-Methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

This example describes a novel preparation of Example 5 above.

A mixture of 0.71 g of ethyl (S)-2-[(quinol-4-ylmethyl)amino]propanoateand 1.42 g of 4-(trifluoromethanesulfanylphenyl) isocyanate in 15 ml ofTHF is stirred for 15 hours at room temperature under an argonatmosphere. After evaporating off the solvent under reduced pressure, 20ml of dichloromethane are added. The precipitate is filtered off. Thefiltrate is concentrated under reduced pressure and the residue ispurified by flash chromatography (SiO₂, CH₂C12 and then CH₂Cl2/MeOH,95/5 by volume as eluent, Ar). 0.69 g of(S)-5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis isolated in the form of a white powder.

[α]_(D)=−33.1°±/0.8 (MeOH)

Mass: EI m/z=431 M+. base peak

m/z=143 [C10H9N]+.

1H NMR spectrum (400 MHz, (CD3)₂SO d6, δ in ppm): 1.42 (d, J=5.5 Hz:3H); 4.35 (q, J=5.5 Hz: 1H); 5.08 (d, J=17 Hz: 1H); 5.25 (d, J=17 Hz:1H); 7.65 (d, J=5 Hz: 1H); from 7.65 to 7.75 (mt: 1H); 7.70 (d, J=8.5Hz: 2H); 7.83 (broad t, J=8 Hz: 1H); 7.89 (d, J=8.5 Hz: 2H); 8.10 (broadd, J=8.5 Hz: 1H); 8.25 (broad d, J=8.5 Hz: 1H); 8.90 (d, J=5 Hz: 1H).

Ethyl (S)-2-[(quinol-4-ylmethyl)amino]propanoate (P-31397-073-1)

A mixture of 2 g of L-alanine ethyl ester in hydrochloride form and 1.83ml of triethylamine in 30 ml of dichloromethane is stirred at roomtemperature for 10 minutes. Next, 2.05 g of quinoline-4-carbaldehyde areadded. The reaction medium is stirred at room temperature for 15 hoursand then concentrated under reduced pressure. 35 ml of ethanol are thenadded; the solution is cooled to 0° C. and 0.49 g of sodium borohydrideis then added portionwise. Stirring is continued for 15 hours at roomtemperature. The precipitate formed is filtered off; the filtrate isconcentrated under reduced pressure. The residue is purified by flashchromatography on a column (SiO₂, CH₂Cl2/MeOH, 95/5 by volume as eluent,Ar). 0.71 g of ethyl (S)-2-[(quinol-4-ylmethyl)amino]propanoate isobtained in the form of a pink oil.

Mass: EI m/z=258 M+.

m/z=185 [M-COOCH2CH₃]+ base peak

m/z=142 [C₁₀H₈N]+

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.22 (t, J=7 Hz: 3H);1.28 (d, J=7 Hz: 3H); 2.72 (unresolved peak: 1H); 3.42 (mt: 1H); from4.00 to 4.20 (mt: 1H); 4.13 (q, J=7 Hz: 2H); 4.27 (broad d, J=16 Hz:1H); 7.55 (broad d, J=5 Hz: 1H); 7.64 (ddd, J=8.5-7.5 and 1 Hz: 1H);7.77 (ddd, J=8.5-7.5 and 1 Hz: 1H); 8.04 (broad d, J=8.5 Hz: 1H); 8.22(broad d, J=8.5 Hz: 1H); 8.86 (d, J=5 Hz: 1H).

EXAMPLE 595,5-Dimethyl-1-quinol-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

This example describes a novel preparation of Example 42 above.

The product is prepared according to the procedure described in Example58 with 600 mg of methyl 2-methyl-2-[(quinol-4-ylmethyl)amino]propanoateinstead of ethyl (S)-2-[(quinol-4-ylmethyl)amino]propanoate used inExample 58 and 1.114 g of 4-(trifluoromethoxyphenyl) isocyanate insteadof 4-(trifluoromethanesulfanylphenyl) isocyanate used in Example 58.After purification by flash chromatography on a column (SiO₂, CH₂Cl2 aseluent, Ar) and then a second purification by flash chromatography on acolumn (SiO2, 60/40 cyclohexane/EtOAc by volume as eluent, Ar), 710 mgof the desired product are obtained.

Mass: EI m/z=429 M+. base peak

m/z=414 [M-CH3]+

m/z=359 [M-C₄H₆₀]⁺.

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.46 (s: 6H); 5.16 (s:2H); 7.55 (broad d, J=8.5 Hz: 2H); 7.65 (d, J=5 Hz: 1H); 7.69 (d, J=8.5Hz: 2H); 7.70 (mt: 1H); 7.83 (ddd, J=8-7.5 and 1.5 Hz: 1H); 8.09 (broadd, J=8.5 Hz: 1H); 8.27 (broad d, J=8.5 Hz: 1H); 8.88 (d, J=5 Hz: 1H).

Preparation of methyl 2-((quinol-4-ylmethyl)amino)propanoate

A mixture of 1.5 g of methyl α-aminoisobutyrate hydrochloride and 1.4 mlof triethylamine in 30 ml of dichloromethane is stirred at 0° C. for 20minutes. Next, 1 g of magnesium sulfate and 1.5 g ofquinoline-4-carbaldehyde are added. Stirring is continued for 15 hoursat room temperature and the mixture is then concentrated under reducedpressure. The residue is taken up in 35 ml of methanol and the solutionobtained is cooled to 0° C. 0.4 g of sodium borohydride is addedportionwise and stirring is continued at room temperature for 15 hours.The precipitate formed is filtered and the filtrate is concentratedunder reduced pressure. The residue obtained is purified byrecrystallization from diisopropyl ether. 600 mg of the expected productare obtained in the form of a pink oil.

Mass: DCI m/z=259 [M+H]+

m/z=199 [M+H—HCOOCH3]+

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.36 (s: 6H); 2.68(broad t, J=7 Hz: 1H); 3.69 (s: 3H); 4.11 (d, J=7 Hz: 2H); 7.60 (broadd, J=5 Hz: 1H); 7.63 (ddd, J=9-8.5 and 1 Hz: 1H); 7.76 (ddd, J=9-8.5 and1 Hz: 1H); 8.03 (broad d, J=8.5 Hz: 1H); 8.20 (broad d, J=8.5 Hz: 1H);8.85 (d, J=5 Hz: 1H).

EXAMPLE 605,5-dimethyl-1-(3-chloro-6-methoxyquinol-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

The product is prepared according to the procedure described in Example59, starting with 180 mg of methyl2-methyl-2-[(3-chloro-6-methoxyquinol-4-ylmethyl)amino]propanoateinstead of methyl 2-methyl-2-[(quinol-4-ylmethyl)amino]propanoate usedin Example 59 and 267 mg of 4-(trifluoromethoxy)phenyl isocyanate. Afterpurification by flash chromatography on a column (SiO2, 80/20cyclohexane/EtOAc by volume as eluent, Ar), 137 mg of the expectedproduct are obtained.

Mass: EI m/z=493 M+. isotopic band of the peak

monochloro m/z=458 [M-Cl]+ base peak

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.27 (s: 6H); 3.89 (s:3H); 5.27 (s: 2H); 7.48 (dd, J=9 and 3 Hz: 1H); 7.56 (broad d, J=8.5 Hz:2H); 7.68 (dt, J=8.5 and 2 Hz: 2H); 7.79 (d, J=3 Hz: 1H); 8.01 (d, J=9Hz: 1H); 8.80 (s: 1H).

Preparation of methyl2-methyl-2-[(3-chloro-6-methoxyquinol-4-ylmethyl)amino]propanoate(P-31397-099-1)

The product is prepared according to the procedure described in Example59, starting with 1 g of methyl α-aminoisobutyrate hydrochloride, 1.25 gof (3-chloro-6-methoxy)quinoline-4-carbaldehyde instead ofquinoline-4-carbaldehyde used in Example 59, 0.66 g of triethylamine and250 mg of sodium borohydride. After purification by flash chromatography(SiO2, 70/30 cyclohexane/EtOAc by volume as eluent, Ar), 180 mg of theexpected product are obtained.

Mass: EI m/z=322 M+. isotopic band of the peak

monochloro m/z=263 [M-COOCH3]+ base peak

isotopic band of the monochloro peak m/z=206 [M-C5H10O2N]+isotopic bandof the monochloro peak

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.39 (s: 6H); 2.47(broad t, J=7.5 Hz: 1H); 3.74 (s: 3H); 3.98 (s: 3H); 4.04 (d, J=7.5 Hz:2H); 7.46 (dd, J=9 and 3 Hz: 1H); 7.66 (d, J=3 Hz: 1H); 7.97 (d, J=9 Hz:1H); 8.71 (s: 1H).

Preparation of (3-chloro-6-methoxyquinoline)-4-carbaldehyde(P-31397-097-1)

A solution of 2 g of 4-bromo-3-chloro-6-methoxyquinoline in 50 ml of THFis cooled to −78° C. 6.9 ml of a 1.6 M solution of nBuLi in dioxane areadded. The solution is stirred for 2 hours at this temperature and 1.7ml of DMF are then added. The mixture is stirred at −60° C. for 2 hours30 minutes and the reaction medium is then allowed to warm to roomtemperature. 200 ml of water are then added. The organic phase isextracted with 200 ml of ethyl acetate, washed with 5×200 ml of water,dried over magnesium sulfate and concentrated under reduced pressure.The residue obtained is purified by flash chromatography on a column(SiO2, 80/20 cyclohexane/EtOAc by volume as eluent, Ar). 1.2 g of theexpected product are obtained in the form of a yellow powder.

Mass: EI m/z=221 M+. base peak, isotopic band of the monochloro

m/z=193 [M-CO]+. isotopic band of the monochloro peak

m/z=150 [M-C₃H₃₀₂]+ isotopic band of the monochloro peak

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 3.96 (s: 3H); 7.56(dd, J=9 and 3 Hz: 1H); 8.07 (d, J=9 Hz: 1H); 8.22 (d, J=3 Hz: 1H); 8.93(s: 1H); 10.77 (s: 1H).

Preparation of 4-bromo-3-chloro-6-methoxyquinoline is described inFrench patent FR 2 816 618 in Example 1.

EXAMPLE 615,5-Dimethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.764 g of 4-(trifluoromethanesulfanylphenyl) isocyanate is added to asolution of 0.726 g of methyl2-methyl-2-[(pyrid-4-ylmethyl)amino]propanoate in 10 ml oftetrahydrofuran. The reaction medium is stirred under an argonatmosphere for about 3 days at a temperature in the region of 20° C. Thereaction mixture is taken up in ethyl acetate, washed successively withwater and then with saturated sodium chloride solution. The organicphase is dried over magnesium sulfate and then concentrated underreduced pressure. The residue thus obtained is purified by flashchromatography on an AIT cartridge of reference FC-50SI filled with 50 gof silica conditioned and eluted with dichloromethane at a flow rate of10 ml per minute. The fractions between 100 and 280 ml are concentratedunder reduced pressure, the residue obtained is taken up in ethyl etherand the insoluble material is filtered off. 700 mg of5,5-dimethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneare thus obtained in the form of a white powder, the characteristics ofwhich are as follows:

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.43 (s: 6H); 4.66 (s:2H); 7.44 (broad d, J=6 Hz: 2H); 7.69 (d t, J=8.5 and 2.5 Hz: 2H); 7.87(broad d, J=8.5 Hz: 2H); 8.55 (dd, J=6 and 1.5 Hz: 2H).

Mass IE m/z=395 M+. base peak

m/z=380 (M-CH₃)+

m/z=219 C₈H₄NOSF3+.

m/z=92 C₆H₆N+

Preparation of methyl 2-methyl-2-[(pyrid-4-ylmethyl)amino]propanoate(P-31402-151-1)

1.04 ml of triethylamine and then 0.659 g of pyridine-4-carbaldehyde aresuccessively added to a solution of 0.945 g of methyl α-aminoisobutyratehydrochloride in 28 ml of dichloroethane. The reaction mixture isstirred overnight at a temperature in the region of 20° C. The mixtureis purified by filtration on Merck Lichroprep aminopropyl-graftedsilica. The filtrate is concentrated under reduced pressure and theresidue thus obtained is taken up in 25 ml of methanol, 0.372 g ofsodium borohydride is added. The reaction mixture is stirred for 48hours at a temperature in the region of 20° C. and then poured into amixture of a normal solution of sodium hydroxide/ice. The mixtureobtained is extracted three times with ethyl acetate. The organic phaseis dried over magnesium sulfate and then concentrated under reducedpressure. 0.726 g of methyl2-methyl-2-[(pyrid-4-ylmethyl)amino]propanoate is thus obtained in theform of an oil, the characteristics of which are as follows:

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.27 (s: 6H); 2.69(broad t, J=5 Hz: 1H); 3.64 (s: 3H); 3.65 (d, J=5 Hz: 2H); 7.35 (broadd, J=6 Hz: 2H); 8.47 (dd, J=6 and 1.5 Hz: 2H).

Mass IC m/z=209 MH+ base peak

m/z=149 (M-C₂H₄O2)+

EXAMPLE 621-Pyrid-4-ylmethyl-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.087 g sodium hydride is added to a solution of 0.300 g of3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione in 6 ml ofanhydrous dimethylformamide, under an inert atmosphere of argon at atemperature in the region of 20° C., stirring is continued at thistemperature for 30 minutes, 0.152 ml of triethylamine and 0.274 g of4-(bromomethyl)pyridine hydrobromide are successively added, followed byaddition of ice-cold water 10 minutes later. The reaction mixture isplaced on a cartridge 37 mm in diameter packed with 50 g of Amicon 50 μmoctadecyl-grafted silica of ref. conditioned successively with awater/acetonitrile mixture (5/95, v/v) and then a water/acetonitrilemixture (95/5, v/v).

The elution was performed with a water/acetonitrile mixture (95/5, v/v)over 20 minutes, followed by a linear gradient from 5% to 95% ofacetonitrile over 60 minutes, at a flow rate of 10 ml/minute. Thefractions between 580 and 630 ml are concentrated under reducedpressure. 0.220 g of1-pyrid-4-ylmethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white powder, the characteristics ofwhich are as follows:

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 4.16 (s: 2H); 4.65 (s:2H); 7.42

(broad d, J=6 Hz: 2H); 7.64 (broad d, J=8.5 Hz: 2H); 7.87 (broad d,J=8.5 Hz: 2H); 8.57 (broad d, J=6 Hz: 2H).

Mass IE m/z=367 M+. base peak

m/z=219 C₈H₄NOSF3+.

m/z=92 C₆H₆N+

The compound 3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis described in patent U.S. Pat. No. 4,496,575.

EXAMPLE 635,5-Dimethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

0.042 g of sodium hydride is added to a solution of 0.150 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione in 3 mlof anhydrous dimethylformamide, under an inert atmosphere of argon andat a temperature in the region of 20° C., stirring is continued at thistemperature for 30 minutes, 0.094 ml of triethylamine and 0.132 g of4-(bromomethyl)pyridine hydrobromide are successively added, followed byaddition of ice-cold water 10 minutes later. The reaction mixture isplaced on a cartridge 27 mm in diameter packed with 30 g of Amicon 50 μmoctadecyl-grafted silica conditioned successively with awater/acetonitrile mixture (5/95, v/v) and then a water/acetonitrilemixture (95/5, v/v). The elution was performed with a water/acetonitrilemixture (95/5, v/v) over 20 minutes, followed by a linear gradient from5% to 95% of acetonitrile over 60 minutes, at a flow rate of 10ml/minute. The fractions between 300 and 450 ml are concentrated underreduced pressure. 0.1 g of mixture is thus obtained, which is repurifiedon a cartridge of 37 mm in diameter packed with 50 g of Amicon 50 μmoctadecyl-grafted silica of ref. conditioned successively with awater/acetonitrile mixture (5/95, v/v) and then a water/acetonitrilemixture (95/5, v/v). The elution was performed with a water/acetonitrilemixture (95/5, v/v) over 20 minutes, followed by a linear gradient from5% to 95% of acetonitrile over 60 minutes, at a flow rate of 10ml/minute. The fractions between 550 and 750 ml are concentrated underreduced pressure. 0.060 g of5,5-dimethyl-1-pyrid-4-ylmethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which are as follows:

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.42 (s: 6H); 4.65 (s:2H); 7.44 (broad d, J=6 Hz: 2H); 7.53 (broad d, J=8.5 Hz: 2H); 7.64 (dt,J=8.5 and 2.5 Hz: 2H); 8.54 (broad d, J=6 Hz: 2H).

Mass IE m/z=379 M+. base peak

m/z=364 (M-CH3)+

m/z=203 C₈H₄NO2F3+.

m/z=92 C₆H₆N+

Preparation of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

A solution of 7.08 g of 4-trifluoromethoxyaniline in 50 ml of toluene isadded over 15 minutes to a suspension of 8.7 g of diphosgene and 1 g ofplant charcoal in 100 ml of toluene, at a temperature in the region of−20° C. The mixture is stirred until the temperature is in the region of20° C., and then refluxed for 3 hours. The mixture is cooled to atemperature in the region of 20° C. and then filtered through Celite, 5g of methyl α-aminoisobutyrate hydrochloride, 50 ml of toluene and 10 mlof triethylamine are added to the filtrate. The mixture thus obtained isrefluxed for 16 hours and then cooled to a temperature in the region of20° C. The precipitate is filtered off and the filtrate is concentratedunder reduced pressure, the residue obtained is purified by flashchromatography on a column packed with silica, conditioned and theneluted with a cyclohexane/ethyl acetate mixture (50/50, v/v). Thefractions containing the expected product are concentrated under reducedpressure, and 3.4 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione arethus obtained, the characteristics of which are as follows:

Mass IE m/z=288 M+. base peak

m/z=273 (M-CH3)+

m/z=203 C₈H₄NO2F3+.

1H NMR spectrum (300 MHz, (CD3)₂SO d6, δ in ppm): 1.42 (s: 6H); 7.49 (d,J=9 Hz: 2H); 7.55 (d, J=9 Hz: 2H); 8.63 (unresolved peak: 1H).

EXAMPLE 64 Preparation of3-[4-(pentafluorothio)phenyl]-5,5-dimethyl-1-quinolin-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.16 mmol of resin, 0.48 mmol ofFmoc-AIB-(OH), 1.12 mmol of 4-quinolinecarboxaldehyde and 0.4 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 5 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 472

EXAMPLE 65 Preparation of3-[4-(pentafluorothio)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.16 mmol of resin, 0.48 mmol ofFmoc-AIB-(OH), 1.12 mmol of 4-pyridinecarboxaldehyde and 0.4 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 13.2 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 422

EXAMPLE 66 Preparation of3-[4-(pentafluorothio)phenyl]-1-quinolin-4-yl-methylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.1 mmol of resin, 0.3 mmol ofN-Fmoc-Gly-(OH), 0.5 mmol of 4-quinolinecarboxaldehyde and 0.25 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 18 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 444

EXAMPLE 67 Preparation of3-[4-(pentafluorothio)phenyl]-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.1 mmol of resin, 0.3 mmol ofN-Fmoc-Gly-(OH), 0.5 mmol of 4-quinolinecarboxaldehyde and 0.25 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 18 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 394

EXAMPLE 68 Preparation of3-[4-(pentafluorothio)phenyl]-1-pyrid-2-ylmethylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.1 mmol of resin, 0.3 mmol ofN-Fmoc-Gly-(OH), 0.5 mmol of 4-quinolinecarboxaldehyde and 0.25 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 9 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 394

EXAMPLE 69 Preparation of3-[4-(pentafluorothio)phenyl]-1-pyrid-3-ylmethylimidazolidine-2,4-dionetrifluoroacetate

The compound is prepared from 0.2 mmol of resin, 0.6 mmol ofN-Fmoc-Gly-(OH), 1 mmol of 4-quinolinecarboxaldehyde and 0.5 mmol of4-(pentafluorothio)aniline, in the same manner as in Example 1. Afterpurification by preparative LC-MS chromatography, 42 mg of the desiredproduct are obtained.

EIMS ([M+H]+): 394

The 6 reaction schemes below describe the preparation of compound offormula I according to the present invention, especially among theproducts of Examples 70 to 178 below.

Scheme 1 describes the preparation of hydantoin derivatives with aminosubstituents in the two positions of the pyridine ring (B2).

Procedures for Scheme 1Step 1:

(Syntheses described for X═S, analogous scheme for X═O).

1-Isocyanato-4-trifluoromethylsulfanylbenzene (14.27 g, 65 mmol) isdissolved in 30 ml of dry CH₂Cl₂ and is cooled to 0° C. 7.5 g (65 mmol)of N-ethylmorpholine are added, followed by addition of 10 g (65 mmol)of methyl 2-amino-2-methylpropionate. The reaction mixture is left toreach 25° C. over a period of 6 hours, washed with water and, afterremoving the solvent, 21.8 g of methyl2-methyl-2-[3-(4-trifluoromethylsulfanylphenyl)-ureido]propionate 3 areisolated.

Step 2:

30 g of 2-methyl-2-[3-(4-trifluoromethylsulfanylphenyl)ureido]propionate3 are dissolved in a mixture of 225 ml of 3 N HCl and 230 ml of dioxane,refluxed for 6 hours and, after cooling to 4° C., the product5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)-imidazolidine-2,4-dioneis isolated in the form of white crystals (24.14 g).

Step 3:

5,5-Dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione3 (1 g, 3.29 mmol) is dissolved in 10 ml of DMF, 1.36 g of K₂CO₃ (3 eq,9.87 mmol) and 909 mg of 2-chloro-4-chloromethylpyridine (3.95 mmol, 1.2eq) are added, and the mixture is refluxed for 20 hours. The solvent isremoved under vacuum and the residue is dissolved in CH₂Cl₂ and treatedthree times with active charcoal. After removing the solvent, theproduct1-(2-chloropyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis obtained (3.2 g; 56%).

Analytical data:

MS (LC-MS): 429.05; retention time: 2.49 min.

NMR: 1.4: s, 6H, 4.7: s, 2H, 7.45: m, 1H, 7.6: s, 1H, 7.7: d, 2H, 7.9:d, 2H, 8.4: m, 1H.

Preparation of 2-chloro-4-chloromethylpyridine

10 g of 2-chloro-4-methylpyridine are dissolved in 30 ml of CH₃CN and amixture of AIBN (3 g) and NCS (30 g) is added. The resulting mixture isrefluxed for 4 hours. After removing the solvent, the crude product isfurther purified by distillation (boiling point: 70° C., 20 mtorr).

Step 4: General Procedure for the Palladium-Catalyzed Amination of thePyridine Ring System in1-(2-chloropyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

100 mg (0.23 mmol) of1-(2-chloropyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione,20 mg of Pd(OAc)₂, 60 mg of XANTPHOS and 300 mg of Cs₂CO₃ aretransferred into a reaction tube with a screw stopper equipped with arubber seal, and an argon atmosphere is generated in the tube. 1.5equivalents (0.35 mmol) of the appropriate amine or amide are dissolvedin 10 ml of toluene, the solution is transferred into the reaction tubementioned above and the resulting mixture is heated at 95° C. for 6 to10 hours depending on the reaction progress, monitored by LCMS.

After filtration, the solvent is removed under vacuum and the crudeproduct is further purified by chromatography on an HPLC system.

Scheme 2 describes the preparation of urea and thiourea derivatives.

Procedures for Scheme 2:Step 1:

This step is identical to step 4 of Scheme 1, with acetamide as reagentin the catalytic reaction.

Analytical data forN-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanyl-phenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamide:

MS (LC-MS): 452.11; retention time: 1.82 min.

NMR: 1.4: s, 6H, 2.05: s, 3H, 4.65: s, 2H, 7.1: m, 1H, 7.65: d, 2H,7.85: d, 2H, 8.15: m, 1H, 8.25: m, 1H.

Step 2:

500 mg (1.11 mmol) ofN-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamideare dissolved in MeOH, 1.5 mmol of NaOMe are added and the resultingmixture is refluxed for 4 hours. The solvent is removed, the residue istaken up in CH₂Cl₂ and washed twice with 10% NaHCO₃ solution and withwater, and the organic phase is evaporated off. 340 mg (75%) of1-(2-aminopyrid-4-yl-methyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneare isolated in this manner.

MS (LC-MS): 410.10; retention time: 1.57.

NMR: 1.4: s, 6H, 4.4: s, 2H, 6.35: s, 2H, 6.4: m, 1H, 6.5: m, 1H, 7.65:d, 2H, 7.9: m, 3H.

Step 3: General Procedure all the Urea and Thiourea Derivatives arePrepared in this Manner.

100 mg of1-(2-aminopyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanyl-phenyl)imidazolidine-2,4-dioneare dissolved in 5 ml of dioxane and 1.5 equivalents of thecorresponding isocyanate or isothiocyanate are added. The reactionmixture is stirred at slightly elevated temperature up to the end, whichis monitored by LCMS. The solvent is removed and further purification isperformed by chromatography on an HPLC system.

Step 1:

(Syntheses Described for X═S. Analogous Scheme for X═O)

5,5-Dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione(1 000 mg/3.29 mmol) is dissolved in 20 ml of DMF, Cs₂CO₃ (3.21 g/9.9mmol) and 2,6-dichloro-4-chloromethylpyridine (774 g/3.9 mmol) are addedand the resulting mixture is heated at 80° C. for 6 hours. The solventis removed and the residue is dissolved in CH₂Cl₂ and washed three timeswith water. After evaporating off the solvent, the crude material isfurther purified by chromatography on an HPLC system.

Step 2: General procedure for the Pd-catalyzed monoamination of1-(2,6-dichloropyrid-4-yl-methyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

This step is identical to step 4 of Scheme 1, but only 1 equivalent ofthe corresponding amine or amide is used.

Step 3: General procedure for the Pd-catalyzed bisamination of1-(2,6-dichloropyrid-4-yl-methyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

This step is identical to step 4 of Scheme 1, but in this case 2.2equivalents of the corresponding amine or amide are used.

5,5-Dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione(100 mg/0.33 mmol) is dissolved in 10 ml of DMF, Cs₂CO₃ (321 mg/0.99mmol) and 0.49 mmol (1.5 equivalents) of the aromatic or aliphaticheterocycle substituted with a corresponding chloromethyl or bromomethylgroup are added and the resulting mixture is heated at 80° C. for 6hours. The solvent is removed and the crude material obtained is furtherpurified by chromatography on an HPLC system.

Syntheses of Examples 175, 176 and 177

100 mg (0.23 mmol) of1-(2-chloropyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione,20 mg of Pd(OAc)₂, 60 mg of XANTPHOS, 300 mg of Cs₂CO₃ and 124 mg ofMo(CO)₆ (2 eq) are transferred into a reaction tube with a screwstopper, equipped with a rubber seal, and an argon atmosphere isgenerated in the tube.

1.5 equivalents (0.35 mmol) of the appropriate amine and 212 mg of DBUare dissolved in 10 ml of toluene, this solution is transferred into thereaction tube mentioned above and the resulting mixture is heated at 95°C. for 6 to 10 hours depending on the reaction progress, which ismonitored by LCMS.

After filtration, the solvent is removed under vacuum and the crudeproduct is further purified by chromatography on an HPLC system.

Synthesis of Example 178

30 mg (0.05 mmol) of methyl2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureido)benzoateare dissolved in 2 ml of MeOH, 0.1 mmol of NaOMe is added and theresulting mixture is stirred overnight at room temperature. Afterevaporating off the solvent, the crude5,5-dimethyl-1-[2-(4-oxo-2-thioxo-1,4-dihydro-2H-quinazolin-3-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis further purified by chromatography on an HPLC system.

EXAMPLE 70N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide;compound with trifluoroacetic acid

MS (LC-MS): 466.13, Retention time: 1.83 min.

NMR: 1.05: t, 3H, 1.40: s, 6H, 2.35: q, 2H, 4.65: s, 2H, 7.1: d, 1H,7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25: d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 71N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}isobutyramide;compound with trifluoroacetic acid

MS (LC-MS): 480.14, Retention time: 1.93 min.

NMR: 1.10: d, 6H, 1.40: s, 6H, 2.75: s, 1H, 4.65: s, 2H, 7.15: d, 1H,7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25: d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 72N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-morpholin-4-ylpropionamide;compound with trifluoroacetic acid

MS (LC-MS): 551.18, Retention time: 1.54 min.

NMR: 1.40: s, 6H, 2.85: m, 2H, 3.1: m, 2H, 3.4: m, 2H, 3.95: m, 2H,4.65: s, 2H, 7.15: d, 1H, 7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25:d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 73N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-[4-(2-hydroxyethyl)piperazin-1-yl]propionamide

MS (LC-MS): 594.22, Retention time: 1.40 min.

NMR: 1.40: s, 6H, 2.55 to 3.50: m, 12H, 4.65: s, 2H, 7.15: m, 1H, 7.65:d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25: d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 74N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-methylpiperazin-1-yl)propionamide

MS (LC-MS): 564.21, Retention time: 1.41 min.

NMR: 1.40: s, 6H, 2.55 to 3.50: m, 12H, 2.75: s, 3H, 4.65: s, 2H, 7.15:m, 1H, 7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25: d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 75{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-cyclopropanecarboxamide

MS (LC-MS): 478.13, Retention time: 1.99 min.

NMR: 0.80: m, 4H, 1.15: t, 1H, 1.40: s, 6H, 4.65: s, 2H, 7.15: m, 1H,7.65: d, 2H; 7.85: d, 2H, 8.15: s, 1H, 8.25: d, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 765,5-dimethyl-1-[2-(pyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 487.13, Retention time: 1.85 min.

NMR: 1.40: s, 6H, 4.65: s, 2H, 7.3: m, 4H, 7.65: d, 2H, 7.85: d, 2H,8.05: s, 1H; 8.35: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 77N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-pyrrolidin-1-ylpropionamide

MS (LC-MS): 535.19, Retention time: 1.52 min.

NMR: 1.40: s, 6H, 1.8: m, 2H, 2.0: m, 2H, 2.85: m, 2H, 3.0: m, 2H, 3.4:m, 2H, 3.5: m, 2H, 4.65: s, 2H, 7.2: m, 1H, 7.65: d, 2H, 7.85: d, 2H,8.15: s, 1H, 8.40: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 785,5-dimethyl-1-{2-[3-(4-methylpiperazin-1-yl)propylamino]pyrid-4-ylmethyl}-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 550.23, Retention time: 1.52 min.

NMR: 1.40: s, 6H, 2.6 to 3.5: m, 14H, 2.75: s, 3H, 4.65: s, 2H, 6.85: m,1H, 6.95: m, 1H, 7.65: d, 2H, 7.9: m, 3H.

The synthesis is described in Scheme 1.

EXAMPLE 795,5-dimethyl-1-{2-[3-(4-ethylpiperazin-1-yl)propylamino]pyrid-4-ylmethyl}-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

The synthesis is described in Scheme 1.

EXAMPLE 801-[2-(3-methoxyphenylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 516.14, Retention time: 1.90 min.

NMR: 1.40: s, 6H, 3.7: s, 3H, 4.65: s, 2H, 6.6: m, 1H, 6.9: m, 2H, 7.15:m, 1H, 7.2: m, 1H, 7.25: m, 1H, 7.65: d, 2H, 7.85: d, 2H, 8.05: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 81N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-ethylpiperazin-1-yl)propionamide

MS (LC-MS): 516.14, Retention time: 1.90 min.

NMR: 1.15: t, 3H, 1.40: s, 6H, 2.5 to 3.7: m, 14H, 4.65: s, 2H, 7.15: m,1H, 7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.25: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 825,5-dimethyl-1-[2-(3-methyl-2-oxopyrrolidin-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 492.14; Retention time: 2.23 min.

NMR: 1.15: d, 3H, 1.40: s, 6H, 1.60: m, 1H, 2.30: m, 1H, 2.70: m, 1H,3.80: m, 1H; 4.0: m, 1H, 4.65: s, 2H, 7.15: m, 1H, 7.65: d, 2H, 7.85: d,2H, 8.35: m, 2H.

The synthesis is described in Scheme 1.

EXAMPLE 83

MS (LC-MS): 495.19; Retention time: 1.43 min.

The synthesis is described in Scheme 1.

EXAMPLE 845,5-dimethyl-1-[2-(4-pyrid-2-ylpiperazin-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 556.19; Retention time: 1.56 min.

The synthesis is described in Scheme 1.

EXAMPLE 85N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-piperid-1-ylpropionamide;compound with trifluoroacetic acid

MS (LC-MS): 549.22; Retention time: 1.62 min.

NMR: 1.45: s, 6H, 1.55: m, 3H, 1.80: m, 2H, 2.80: m, 4H, 3.3 to 3.5: m,7H, 4.65: s, 2H, 7.15: m, 1H, 7.65: d, 2H, 7.85: m, 2H, 8.15: m, 1H,8.3: m, 1H, 9.0: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 861-[2-(3-imidazol-1-ylpropylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 518.17; Retention time: 1.57 min.

The synthesis is described in Scheme 1.

EXAMPLE 871-[2-(4-ethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 515.16; Retention time: 1.85 min.

NMR: 1.15: t, 3H, 1.45: s, 6H, 2.7: q, 2H, 4.75: s, 2H, 7.1: broad s,2H, 7.3: broad s 2HM; 7.65: d, 2H, 7.85: d, 2H, 8.25: s, 1H, 8.45: s,1H.

The synthesis is described in Scheme 1.

EXAMPLE 881-[2-(6-ethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 515.16; Retention time: 1.95 min.

NMR: 1.15: t, 3H, 1.45: s, 6H, 2.7: q, 2H, 4.75: s, 2H, 7.1: broad s,2H, 7.3: broad s 2HM; 7.65: d, 2H, 7.85: d, 2H, 8.25: s, 1H, 8.45: s,1H.

The synthesis is described in Scheme 1.

EXAMPLE 895,5-dimethyl-1-[2-(quinolin-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 537.14; Retention time: 1.95 min.

NMR: 1.45: s, 6H, 4.75: s, 2H, 7.4 to 7.6: m, 6H, 7.65: d, 2H, 7.85: d,2H, 8.00: broad s, 1H, 8.50: broad s, 2H.

The synthesis is described in Scheme 1.

EXAMPLE 905,5-dimethyl-1-[2-(4-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 501.14; Retention time: 1.80 min.

NMR: 1.45: s, 6H, 2.4: s, 3H, 4.75: s, 2H, 7.1: m, 2H, 7.25: m, 2H,7.65: d, 2H, 7.85: d, 2H, 8.20: broad s, 1H, 8.45: broad s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 915,5-dimethyl-1-[2-(6-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 501.14; Retention time: 1.85 min.

NMR: 1.45: s, 6H; 2,55: s, 3H, 4.75: s, 2H, 7.1: m, 1H, 7.25: m, 2H,7.4: s, 1H, 7.65: d, 2H, 7.85: m, 3H, 8.45: broad s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 921-[2-(3,5-dichloropyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 555.05; Retention time: 1.96 min.

NMR: 1.45: s, 6H, 4.70: s, 2H, 7.1: m, 1H, 7.20: m, 1H, 7.65: d, 2H,7.85: m, 3H; 8.30: m, 3H.

The synthesis is described in Scheme 1.

EXAMPLE 931-[2-(4,6-dimethylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 515.16; Retention time: 2.00 min.

NMR: 1.45: s; 2.35: s, 3H, 2.6: s, 3H; 6H, 4.75: s, 2H, 7.0: m, 2H,7.35: m, 2H, 7.70: d, 2H, 7.9: d, 2H, 8.40: broad s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 945,5-dimethyl-1-[2-(methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 501.14; Retention time: 1.74 min.

The synthesis is described in Scheme 1.

EXAMPLE 955,5-dimethyl-1-[2-(pyrid-4-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 487.13; Retention time: 1.69 min.

NMR: 1.45: s; 4.70: s, 2H, 7.15: m, 1H, 7.25: m, 1H, 7.65: d, 2H, 7.9:d, 2H, 8.10: broad s, 2H, 8.40: s, 1H, 8.50: m, 2H.

The synthesis is described in Scheme 1.

EXAMPLE 965,5-dimethyl-1-[2-(pyrid-3-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 487.13; Retention time: 1.69 min.

NMR: 1.45: s; 4.60: s, 2H, 6.95: s, 1H, 7.05: s, 1H, 7.7: d, 2H, 7.8: m,1H, 7.85: d, 2H, 8.25: s, 1H, 8.35: s, 1H, 8.45: m, 1H, 9.4: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 97N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2-oxoazepan-1-yl)propionamide

MS (LC-MS): 577.20; Retention time: 2.00 min.

NMR: 1.45: s, 6H, 1.5: m, 4H, 1.55: m, 2H, 2.35: m, 2H, 2.6: m, 4H, 3.3m, 2H; 4.65: s, 2H, 7.15: s, 1H, 7.65: d, 2H, 7.85: d, 2H, 8.1: s, 1H,8.35: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 983-(benzylmethylamino)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide

MS (LC-MS): 585.20, Retention time: 1.73 min.

NMR: 1.45: s, 6H, 2.2: s, 3H, 2.95: m, 2H, 3.3: m, 1H, 4.3: m, 1H, 4.4:m, 1H, 4.65: s, 2H, 7.2: s, 1H, 7.45: m, 2H, 7.50: m, 2H, 7.65: d, 2H,7.85: d, 2H, 8.1: m, 1H, 8.3: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 99N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-pyrrolidin-1-ylacetamide

MS (LC-MS): 521.17, Retention time: 1.68 min.

NMR: 1.45: s, 6H, 1.85: m, 2H, 2.00: m, 2H, 3.1: m, 2H, 4.25: m, 2H,4.7: s, 2H, 7.25: m, 1H, 7.65: d, 2H, 7.85: d, 2H, 8.1: broad s, 1H,8.3: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 100N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-(4-pyrid-2-ylpiperazin-1-yl)acetamide

MS (LC-MS): 613.21, Retention time: 1.60 min.

NMR: 1.45: s, 6H, 3.3: broad m, 4H, 4.35: broad m, 4H, 4.65: s, 2H, 6.7:m, 1H, 6.9: m, 1H, 7.25: s, 1H, 7.65, m+d: 3H, 7.85: d, 2H, 8.15: m, 2H,8.35: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1012-[(2-dimethylaminoethyl)methylamino]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamide

MS (LC-MS): 552.21, Retention time: 1.52 min.

NMR: 1.45: s, 6H, 2.75: s, 6H, 4.65: s, 2H, 7.20: m, 1H, 7.65: d, 2H,7.85: d, 2H, 8.15: s, 1H, 8.30: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1023-[(2-dimethylaminoethyl)methylamino]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}propionamide

MS (LC-MS): 566.23, Retention time: 1.37 min.

NMR: 1.45: s, 6H, 2.75: s, 6H, 2.8 to 3.4: broad m, 8H, 7.20: m, 1H,7.65: d, 2H, 7.85: d, 2H, 8.15: s, 1H, 8.30: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1035,5-dimethyl-1-[2-(5-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 501.14, Retention time: 1.83 min.

NMR: 1.45: s, 6H, 2.3: s, 3H, 4.7: s, 2H, 7.3: m, 3H, 7.7: d, 2H, 7.9:d, 2H, 8.2: m, 1H, 8.35: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 104N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3,5-dimethoxybenzamide;compound with trifluoroacetic acid

MS (LC-MS): 574.78, Retention time: 2.34 min.

NMR: 1.45: s, 6H, 2.3: s, 3H, 4.7: s, 2H, 6.7: s, 2H, 7.2: m, 2H, 7.25:m, 1H, 7.7: d, 2H, 7.9: d, 2H, 8.2: m, 1H, 8.3: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1052-(benzylmethylamino)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamide;compound with trifluoroacetic acid

MS (LC-MS): 574.78, Retention time: 2.34 min.

NMR: 1.45: s, 6H, 2.8: s, 4.0 to 4.4: m, 4H, 4.7: s, 2H, 7.2: m, 1H,7.4: m, 2H, 7.5: m, 2H, 7.7: d, 2H, 7.9: d, 2H, 8.1: m, 1H, 8.3: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1065,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 488.12, Retention time: 1.63.

NMR: 1.45: s, 6H, 4.7: s, 2H, 7.1: m, 1H, 7.6: m, 1H, 7.65: d, 2H, 7.9:d, 2H, 8.2: s, 1H, 8.3: m, 2H, 9.0: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 107N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-phenylbutyramide;compound with trifluoroacetic acid

MS (LC-MS): 566.18, Retention time: 2.43.

NMR: 0.7: t, 3H, 1.4: s, 6H, 1.7: m, 1H, 2.05: m, 1H, 4.6: s, 2H, 7.1:s, 1H, 7.25: m, 1H, 7.3: m, 1H, 7.4: m, 2H, 7.65: d, 2H, 7.85: d, 2H,8.15: s, 1H, 8.25: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 108N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3-methylpiperid-1-yl)propionamide;compound with trifluoroacetic acid

MS (LC-MS): 563.22, Retention time: 1.62.

The synthesis is described in Scheme 1.

EXAMPLE 1091-[2-(4-methoxyphenylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 517.1; Retention time: 1.74.

NMR: 1.4: s, 6H, 4.6: s, 2H, 6.85: broad s, 1H, 7.0: m, 1H, 7.4: m, 2H,7.6: d, 2H, 7.9: d, 2H, 8.95: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1105,5-dimethyl-1-[2-(2-oxopyrrolidin-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 478.13; Retention time: 1.83.

The synthesis is described in Scheme 1.

EXAMPLE 111{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-pyrazine-2-carboxamide;compound with trifluoroacetic acid

MS (LC-MS): 516.12; Retention time: 2.42.

NMR: 1.4: s, 6H, 4.7: s, 2H, 7.3: m, 1H, 7.65: d, 2H, 7.95: d, 2H, 8.3:s, 1H, 8.4: s, 1H, 8.7: s, 1H, 9.0: s, 1H, 9.4: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 112N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2,2-dimethylpropionamide;Compound with Trifluoroacetic Acid

MS (LC-MS): 494.16; Retention time: 2.48.

NMR: 1.2: s, 9H, 1.4: s, 6H, 4.7: s, 2H, 7.2: m, 1H, 7.65: d, 2H, 7.90:d, 2H, 8.1: s, 1H, 8.3: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 113{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-thiophene-2-carboxamide;compound with trifluoroacetic acid

MS (LC-MS): 520.09; Retention time: 2.14.

NMR: 1.4: s, 6H, 4.7: s, 2H, 7.2: m, 2H, 7.65: d, 2H, 7.8: m, 3H, 8.2:s, 1H, 8.25: s, 1H, 8.4: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 114N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-4-methylbenzamide;compound with trifluoroacetic acid

MS (LC-MS): 528.16; Retention time: 2:23.

NMR: 1.4: s, 6H; 4.7: s 2H, 7.2: m, 1H; 7.3: d, 2H; 7.7: d, 2H; 7.85: d,2H; 7.95: d, 2H; 8.2: s, 1H; 8.3: s, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 115N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(3,5-dimethylpiperid-1-yl)propionamide;compound with trifluoroacetic acid

MS (LC-MS): 577.23; Retention time: 1.72.

The synthesis is described in Scheme 1.

EXAMPLE 116N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(4-pyrid-2-ylpiperazin-1-yl)propionamide;compound with trifluoroacetic acid

MS (LC-MS): 627.22; Retention time: 1.50.

NMR: 1.4: s, 6H, 2.9: m, 2H, 3.1: m, 2H, 3.4: m, 2H, 3.6: m, 2H, 4.4: m,2H, 4.65: s, 2H, 6.7: m, 1H, 6.95: d, 1H, 7.2: m, 1H, 7.7: d, 2H, 7.9:d, 2H, 8.15: m, 2H, 8.3: m, 1H.

The synthesis is described in Scheme 1.

EXAMPLE 1175,5-dimethyl-1-[2-(5-trifluoromethylpyrid-2-ylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 555.51; Retention time: 1.78.

The synthesis is described in Scheme 1.

EXAMPLE 118N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-methoxybenzamide;compound with trifluoroacetic acid

MS (LC-MS): 544.14; Retention time: 2.15.

The synthesis is described in Scheme 1.

EXAMPLE 1191-(3,5-dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 597.06; Retention time: 2.15 min.

The synthesis is described in Scheme 2.

EXAMPLE 120 Methyl3-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureido)benzoate

MS (LC-MS): 603.12; Retention time: 2.81 min.

The synthesis is described in Scheme 2.

EXAMPLE 1211-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-phenylurea

MS (LC-MS): 529.14; Retention time: 2.33 min.

NMR: 1.50: s, 6H, 4.65: s, 1H, 7.0: m, 2H, 7.30: m, 2H, 7.5: m, 3H,7.65: d, 2H, 7.85: d, 2H, 8.25: d, 1H, 9.4: s, 1H.

The synthesis is described in Scheme 2.

EXAMPLE 1221-(2,4-dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 597.06; Retention time: 3.00 min.

The synthesis is described in Scheme 2.

EXAMPLE 1231-(3-chlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thiourea

MS (LC-MS): 579.08; Retention time: 3.05 min.

The synthesis is described in Scheme 2.

EXAMPLE 124 Methyl2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureido)benzoate

MS (LC-MS): 603.12; Retention time: 2.85 min.

The synthesis is described in Scheme 2.

EXAMPLE 1253,5-diacetoxy-2-acetoxymethyl-6-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureido)tetrahydropyran-4-ylacetate

MS (LC-MS): 799.18, Retention time: 2.60 min.

The synthesis is described in Scheme 2.

EXAMPLE 1261-(4-dimethylaminophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thiourea

MS (LC-MS): 588.16; Retention time: 1.99.

NMR: 1.4: s, 6H, 2.9: s, 6H, 4.7: s, 2H, 6.7: d, 2H, 7.1: m, 1H, 7.25:s, 1H, 7.4: d, 2H, 7.7: d, 2H, 7.9: d, 2H, 8.25: m, 1H.

The synthesis is described in Scheme 2.

EXAMPLE 1271-(2,4-dimethoxyphenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 589.60; Retention time: 1.98.

The synthesis is described in Scheme 2.

EXAMPLE 1283-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}thioureido)benzoicacid

MS (LC-MS): 589.11; Retention time: 2.30.

The synthesis is described in Scheme 2.

EXAMPLE 1291-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-(2-methoxyphenyl)urea

MS (LC-MS): 559.15; Retention time: 1.88.

The synthesis is described in Scheme 2.

EXAMPLE 1301-(2-aminopyrid-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 4110.0; Retention time: 1.57.

NMR: 1.4: s, 6H, 4.6: s, 2H, 6.9: d, 1H, 7.0: s, 1H, 7.7: d, 2H, 7.85:d, 2H, 7.95: d, 1H, 8.0: broad s, 1H.

The synthesis is described in Scheme 2.

EXAMPLE 1311-(2,6-dichloropyrid-4-yl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imida-zolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 599.42; Retention time: 2.73 min.

NMR: 1.40, s, 6H, 4.65 s, 2H, 7.15: m, 1H, 7.65: d, 2H, 7.85: d, 2H,8.15: s, 1H, 8.25: m, 1H.

The synthesis is described in Scheme 2.

EXAMPLE 1321-(2,6-dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 597.06; Retention time: 2.44 min.

The synthesis is described in Scheme 2.

EXAMPLE 1331-(2,3-dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}urea

MS (LC-MS): 597.06; Retention time: 2.08 min.

The synthesis is described in Scheme 2.

EXAMPLE 1341-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-3-pyrid-3-ylthiourea

MS (LC-MS): 546.11; Retention time: 1.89 min.

The synthesis is described in Scheme 2.

EXAMPLE 1351-[2-chloro-6-(4-methylthiazol-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 541.06; Retention time: 2.49 min.

The synthesis is described in Scheme 3.

EXAMPLE 136N-{6-chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}-2-phenylbutyramide

MS (LC-MS): 541.06; Retention time: 2.49 min.

The synthesis is described in Scheme 3.

EXAMPLE 137N-{6-acetylamino-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamide

MS (LC-MS): 509.13; Retention time: 1.73 min.

The synthesis is described in Scheme 3.

EXAMPLE 1381-[2-chloro-6-(4-methylpyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 535.11; Retention time: 1.90 min.

The synthesis is described in Scheme 3.

EXAMPLE 1391-[2,6-bis(3-methoxyphenylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imida-zolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 621.22; Retention time: 1.95 min.

The synthesis is described in Scheme 3.

EXAMPLE 1401-[2,6-bis(2,4-dimethoxyphenylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 681.24; Retention time: 1.83 min.

The synthesis is described in Scheme 3.

EXAMPLE 1411-[2,6-bis(4-methoxyphenylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imida-zolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 621.22; Retention time: 1.63 min.

The synthesis is described in Scheme 3.

EXAMPLE 142N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethoxyphenyl)imidazolidin-1-ylmethyl]-6-estobutyrylaminopyrid-2-yl}isobutyramide;compound with trifluoroacetic acid

MS (LC-MS): 549.22; Retention time: 1.83 min.

The synthesis is described in Scheme 3.

EXAMPLE 1431-[2-chloro-6-(pyrid-4-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imida-zolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 563.19; Retention time: 2.61 min.

The synthesis is described in Scheme 3.

EXAMPLE 1441-[2-chloro-6-(pyrid-4-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 521.09; Retention time: 1.91 min.

The synthesis is described in Scheme 3.

EXAMPLE 145N-{6-chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyridin-2-yl}propionamide

MS (LC-MS): 500.09; Retention time: 2.46.

The synthesis is described in Scheme 3.

EXAMPLE 146N-{6-chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}acetamide

MS (LC-MS): 486.90; Retention time: 2.15.

The synthesis is described in Scheme 3.

EXAMPLE 1471-[2-chloro-6-(pyrid-3-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imida-zolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 505.11; Retention time: 2.27.

The synthesis is described in Scheme 3.

EXAMPLE 148{6-chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}cyclopropanecarboxamide

MS (LC-MS): 512.09; Retention time: 2.32.

The synthesis is described in Scheme 3.

EXAMPLE 149N-{6-chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyrid-2-yl}isobutyramide

MS (LC-MS): 514.11; Retention time: 1.63.

The synthesis is described in Scheme 3.

EXAMPLE 1501-[2,6-bis(pyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;compound with trifluoroacetic acid

MS (LC-MS): 563.15; Retention time: 1.70 min.

The synthesis is described in Scheme 3.

EXAMPLE 1511-[2-chloro-6-(pyrid-2-ylamino)pyrid-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 521.09; Retention time: 1.78 min.

The synthesis is described in Scheme 3.

EXAMPLE 1525,5-dimethyl-1-(5-phenyl[1,2,4]oxadiazol-3-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 462.10; Retention time: 2.77 min.

The synthesis is described in Scheme 4.

EXAMPLE 1531-(2-imidazol-1-ylethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 398.10; Retention time: 1.49 min.

The synthesis is described in Scheme 4.

EXAMPLE 1541-[2-(4-chlorophenyl)oxazol-5-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 495.06; Retention time: 2.99 min.

The synthesis is described in Scheme 4.

EXAMPLE 155 Preparation of1-isoquinolin-5-yl-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

500 mg (2.4 mmol) of 2-(isoquinolin-5-ylamino)-2-methylpropionitrile,1.6 mg (0.013 mmol) of benzoic acid and 526 mg (2.4 mmol) of4-(trifluoromethylthio)phenyl isocyanate in 4 ml of chlorobenzene wererefluxed for 2 days. The resulting mixture was filtered and the filtratewas evaporated to dryness. The intermediate imine was separated out bypreparative HPLC chromatography (RP 18, acetonitrile, water, 0.01% TFA).60 mg of the resulting product were stirred for 1 hour at 40° C. with 1Nhydrochloric acid. The solvent was evaporated off and the residue wastaken up in sodium hydrogen carbonate solution and extracted with ethylacetate. The combined organic phases were dried and the residueremaining after evaporation was purified by flash chromatography (SiO₂,methylene chloride/methanol=98/2), to give 38 mg of the desired product.

M+H⁺=432.

LC/MS Retention time=1.245.

EXAMPLE 1565,5-dimethyl-1-(5-phenyloxazol-4-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 461.10, Retention time: 2.63 min.

The synthesis is described in Scheme 4.

EXAMPLE 1575,5-dimethyl-1-(1-methylpiperid-3-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 415.15; Retention time: 1.63.

The synthesis is described in Scheme 4.

EXAMPLE 1585,5-dimethyl-1-(1-methylpiperid-3-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

MS (LC-MS): 499.18; Retention time: 1.39.

The synthesis is described in Scheme 4.

EXAMPLE 1591-[2-(4-chlorophenyl)thiazol-4-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imida-zolidine-2,4-dione

MS (LC-MS): 511.04; Retention time: 3.12.

The synthesis is described in Scheme 4.

EXAMPLE 1605,5-dimethyl-1-(1-methyl-1H-imidazol-2-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 398.10; Retention time: 1.53.

The synthesis is described in Scheme 4.

EXAMPLE 1611-(7-methoxy-2-oxo-2H-chromen-4-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 492.48; Retention time: 1.84.

The synthesis is described in Scheme 4.

EXAMPLE 1625,5-dimethyl-1-(5-methylestoxazol-3-ylmethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 500.09; Retention time: 2.52.

The synthesis is described in Scheme 4.

EXAMPLE 163 1-[5-(4-methoxyphenyl)[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 492.11; Retention time: 1.87.

The synthesis is described in Scheme 4.

EXAMPLE 164 1-[5-(4-methoxyphenyl)[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imida-zolidine-2,4-dione

MS (LC-MS): 476.13; Retention time: 2.03.

The synthesis is described in Scheme 4.

EXAMPLE 165 Methyl5-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]-furan-2-carboxylate

MS (LC-MS): 442.42; Retention time: 1.74.

The synthesis is described in Scheme 4.

EXAMPLE 1661-(1-benzyl-1H-imidazol-2-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 474.13; Retention time: 2.02.

The synthesis is described in Scheme 4.

EXAMPLE 1671-(4-dimethylaminopyrimidin-2-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 439.46; Retention time: 1.91.

The synthesis is described in Scheme 4.

EXAMPLE 1681-[1-(4-methoxybenzyl)-1H-imidazol-2-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 504.14; Retention time: 2.24.

The synthesis is described in Scheme 4.

EXAMPLE 1695,5-dimethyl-1-[2-(1-methylpyrrolidin-2-yl)-ethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 415.15; Retention time: 1.66 min.

The synthesis is described in Scheme 4.

EXAMPLE 1705,5-dimethyl-1-(2-morpholin-4-ylethyl)-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 417.13; Retention time: 1.62 min.

The synthesis is described in Scheme 4.

EXAMPLE 171 1-[5-(2-methoxyphenyl)[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 492.11; Retention time: 2.67 min.

The synthesis is described in Scheme 4.

EXAMPLE 1725,5-dimethyl-1-(5-methylestoxazol-3-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

MS (LC-MS): 383.33; Retention time: 1.95 min.

The synthesis is described in Scheme 4.

EXAMPLE 1731-(5-tert-butyl[1,2,4]oxadiazol-3-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 442.16; Retention time: 2.64 min.

The synthesis is described in Scheme 4.

EXAMPLE 1744-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin—ylmethyl]pyridine-2-carboxylicacid 4-methylbenzylamide; compound with trifluoroacetic acid

MS (LC-MS): 542.16; Retention time: 2.80 min.

The synthesis is described in Scheme 5.

EXAMPLE 1754-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyridine-2-carboxylicacid (2-p-tolylethyl)amide

MS (LC-MS): 556.18; Retention time: 2.31.

The synthesis is described in Scheme 5.

EXAMPLE 1764-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyridine-2-carboxylicacid 3,4-dimethoxybenzylamide

MS (LC-MS): 588.16; Retention time: 1.58.

The synthesis is described in Scheme 5.

EXAMPLE 1774-[5,5-dimethyl-2,4-dioxo-3-(4-trifluoromethylsulfanylphenyl)imidazolidin-1-ylmethyl]pyridine-2-carboxylicacid benzylamide

MS (LC-MS): 528.14; Retention time: 1.77.

The synthesis is described in Scheme 5.

EXAMPLE 1785,5-dimethyl-1-[2-(4-oxo-2-thioxo-1,4-dihydro-2H-quinazolin-3-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

MS (LC-MS): 571.10; Retention time: 2.3.

The synthesis is described in Scheme 6 below.

The two reaction schemes below describe the synthesis of compound offormula I according to the present invention, especially among theproducts of Examples 178 to 200 below.

Bis(4-amino-2-chlorophenyl) disulfide

76.8 g (0.4 mol) of 1,2-dichloro-4-nitrobenzene, suspended in 120 ml ofwater, were heated to 90° C. and treated with a solution of 62.4 g (0.8mol) of sodium sulfide and 12.8 g (0.4 mol) of sulfur in 200 ml ofwater.

After refluxing the mixture for 5 hours, 6 g of carbon dioxide werebubbled through the solution, followed by a regular stream of air. ThepH was adjusted to 5.5, the mixture was cooled to room temperature andthe resulting precipitate was collected by filtration.

The crude material was recrystallized from isopropanol to give 45 g(71%) of the desired product.

M+H⁺=318.

LC/MS retention time=1.526.

Bis[(2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyrid-4-ylmethylimidazolidin-1-yl)]phenyldisulfide

A solution of 13.7 g (69.5 mmol) of diphosgene in 100 ml of toluene wascooled to −20° C. and treated with a solution of 5.0 g (15.8 mmol) ofbis(4-amino-2-chlorophenyl) disulfide. The resulting mixture was stirredfor 30 minutes at room temperature, refluxed for 1 hour and thenevaporated to dryness.

2.53 g (about 6.86 mmol) of this material were dissolved in THF andtreated with 2.0 g (9.5 mmol) of methyl2-methyl-2-[(pyrid-4-ylmethyl)amino]propionate. The mixture was stirredfor 3 hours at room temperature and evaporated to dryness, and theresulting solid was purified by flash chromatography (SiO₂, methylenechloride:methanol=97:3) to give 1.8 g (37%) of the desired product.

M+H⁺=722.

LC/MS retention time=1.176.

EXAMPLE 179 Preparation of3-(4-tert-butylsulfanyl-3-chlorophenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

200 mg (0.28 mol) ofbis[(2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyrid-4-yl-methylimidazolidin-1-yl)]phenyldisulfide were dissolved in 10 ml of methanol and treated with 22 mg(0.56 mmol) of sodium borohydride. After stirring for 30 minutes at roomtemperature, the mixture was evaporated to dryness. The residue wasdissolved in 10 ml of sulfuric acid (75%) and added to 20 ml of sulfuricacid (75%) saturated with isobutylene. The mixture was stirred for 20minutes at room temperature and then added cautiously to a cooledsolution of sodium hydroxide in water. The alkaline aqueous phase wasextracted three times with ethyl acetate, the combined organic phaseswere dried with sodium sulfate and the material remaining afterevaporation was filtered off on silica gel (methylenechloride/methanol=95/5). The resulting crude product was purified bypreparative HPLC chromatography (RP 18, acetonitrile, water, 0.01% TFA)to give 120 mg (81%) of the desired product.

M+H⁺=418.

LC/MS retention time=1.249.

General Procedure 1A Preparation of3-(3-chloro-4-alkylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-diones

445 mg (0.62 mol) ofbis[(2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyrid-4-yl-methylimidazolidin-1-yl)]phenyldisulfide were dissolved in 15 ml of methanol and treated with 49 mg(1.24 mmol) of sodium borohydride. After stirring for 30 minutes at roomtemperature, 1.24 mmol of the respective alkyl halide were added and theresulting mixture was refluxed for 1 hour. The solvent was removed byevaporation and the remaining crude materials were purified bypreparative HPLC chromatography (RP 18, acetonitrile, water, 0.01% TFA).

EXAMPLE 180 Preparation of3-(3-chloro-4-isopropylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

Synthesis according to the general procedure 1A.

M+H⁺=404.

LC/MS retention time=1.196.

EXAMPLE 181 Preparation of3-(3-chloro-4-isobutylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=418.

LC/MS retention time=1.272.

EXAMPLE 182 Preparation of3-(3-chloro-4-methylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

Prepared according to the general procedure 1A.

M+H⁺=376.

LC/MS retention time=1.054.

EXAMPLE 183 Preparation of3-[3-chloro-4-(3-methoxypropylsulfanyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=434.

LC/MS retention time=1.096.

EXAMPLE 184 Preparation of3-[3-chloro-4-(2-morpholin-4-ylethylsulfanyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=475.

LC/MS retention time=0.792

EXAMPLE 185 Preparation of3-{3-chloro-4-[2-(1-methylpyrrolidin-2-yl)ethylsulfanyl]phenyl}-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=473.

LC/MS retention time=0.865.

EXAMPLE 186 Preparation of3-{3-chloro-4-[3-(4-methylpiperazin-1-yl)propylsulfanyl]-phenyl}-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=502.

LC/MS retention time=0.795.

EXAMPLE 187 Preparation of3-[3-chloro-4-(3-hydroxypropylsulfanyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=420.

LC/MS retention time=0.968.

EXAMPLE 188 Preparation of3-[3-chloro-4-(2-hydroxyethylsulfanyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=406.

LC/MS retention time=0.921.

EXAMPLE 189 Preparation of[2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyrid-4-ylmethyl-imidazolidin-1-yl)phenylsulfanyl]acetonitriletrifluoroacetate

Prepared according to the general procedure 1A.

M+H⁺=401.

LC/MS retention time=0.999.

3-nitro-4-trifluoromethoxyaniline

20 g (112.9 mmol) of 4-trifluoromethoxyaniline were dissolved in 50 mlof concentrated sulfuric acid at a temperature of 0 to 5° C., treatedwith 30 ml of a 4/1 mixture of sulfuric acid and nitric acid. Themixture was stirred for 5 hours at 0° C. and then poured into anice-cold water mixture and made alkaline with 200 ml of concentratedaqueous ammonia solution. Extraction with EE, drying with sodiumsulfate, evaporation to dryness and recrystallization from ethylacetate/heptane gave 15.5 g (63%) of the desired product.

M+H⁺=223.

LC/MS retention time=1.378.

EXAMPLE 190 Preparation of trifluoroacetic acid;5,5-dimethyl-3-(3-nitro-4-trifluoromethoxyphenyl)-1-pyrid-4-ylmethylimidazolidine-2,4-dione

2.27 g (11.5 mmol) of diphosgene in 1,2-dichloroethane were added at−20° C. to 1.0 g (4.5 mmol) of 3-nitro-4-trifluoromethoxyaniline,dissolved in 20 ml of 1,2-dichloroethane. The mixture was stirred for 1hour while warming to room temperature and was then heated at 50° C. for2 hours. After leaving to stand overnight, the solvent was evaporatedoff and the residue was taken up in dry THF and treated with 937 mg (4.5mmol) of methyl 2-methyl-2-[(pyrid-4-ylmethyl)amino]propionate. Themixture was stirred for 2 hours at room temperature and for 1 hour at40° C., and then evaporated to dryness and the remaining residue waspurified (RP 18, acetonitrile, water, 0.01% TFA) to give 1.15 g (61%) ofthe desired product.

M+H⁺=425.

LC/MS retention time=1.324.

EXAMPLE 191 Preparation of3-(3-amino-4-trifluoro-methoxyphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

9.63 g (22.7 mmol) of5,5-dimethyl-3-(3-nitro-4-trifluoromethoxyphenyl)-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate were dissolved in semi-concentrated hydrochloric acid,heated to reflux and treated with 30 g of zinc powder. After 1.5 hours,the mixture was cooled, filtered and extracted twice with methyltert-butyl ether. The aqueous phase was made alkaline with 6 N sodiumhydroxide and extracted with methyl tert-butyl ether, and the combinedorganic phases were dried over sodium sulfate. Evaporation of thesolvent gave 5.0 g (56%) of the desired product.

M+H⁺=395.

LC/MS retention time=0.948.

EXAMPLE 192 Preparation of5,5-dimethyl-1-pyrid-4-ylmethyl-3-[4-(2,2,2-trifluoroethoxy)phenyl]imidazolidine-2,4-dione

688 mg (3.6 mmol) of 2,2,2-trifluoroethoxyaniline in 30 ml of methylenechloride were added at 0° C. to 356 mg (3.6 mmol) of triethylamine and asolution of 356 mg (1.2 mmol) of triphosgene in 30 ml of methylenechloride. The mixture was stirred overnight while warming to roomtemperature. Next, the solvent was evaporated off, the residue was takenup in 15 ml of THF and treated with 100 mg (0.48 mmol) of methyl2-methyl-2-[(pyrid-4-ylmethyl)amino]propionate and 48.5 mg (0.48 mmol)of triethylamine. The mixture was stirred for 4 hours at roomtemperature and for 1 hour at 50° C., and then evaporated to dryness,and the remaining residue was purified by preparative HPLCchromatography (RP 18, acetonitrile, water, 0.01% TFA) to give 67 g(36%) of the desired product.

M+H⁺=394.

LC/MS retention time=1.032.

EXAMPLE 193 Preparation of3-(8-chloro-3,4,4-trimethylthiochroman-6-yl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

200 mg (0.28 mol) ofbis[(2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyrid-4-yl-methylimidazolidin-1-yl)]phenyldisulfide were dissolved in 10 ml of methanol and treated with 22 mg(0.56 mmol) of sodium borohydride. After stirring for 30 minutes at roomtemperature, the mixture was evaporated to dryness. The residue wasdissolved in 10 ml of sulfuric acid (75%) and added to 20 ml of sulfuricacid (75%) saturated with isobutylene. The mixture was stirred for 30minutes at 40° C., while a regular airstream of isobutylene was bubbledthrough the solution. After leaving to stand overnight, the mixture wasadded cautiously to a cooled solution of sodium hydroxide in water. Thealkaline aqueous phase was extracted three times with ethyl acetate, thecombined organic phases were dried over sodium sulfate and the materialremaining after evaporation was filtered on silica gel (methylenechloride/methanol=95/5). The resulting crude product was purified bypreparative HPLC chromatography (RP 18, acetonitrile, water, 0.01% TFA)to give 70 mg (56%) of the desired product.

M+H⁺=444.

LC/MS retention time=1.240.

EXAMPLE 194 Preparation of1-(2-chlorothiazol-5-ylmethyl)-5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionetrifluoroacetate

200 mg (0.65 mmol) of5,5-dimethyl-3-(4-trifluoro-methylsulfanylphenyl)imidazolidine-2,4-dione,115 mg (0.82 mmol) of potassium carbonate and 276 mg (1.64 mmol) of2-chloro-5-chloromethylthiazole were dissolved in 2 ml of DMF andstirred at room temperature for 2 days. The mixture was poured intowater, extracted three times with ethyl acetate, the combined organicphases were dried over sodium sulfate and the material remaining afterevaporation was purified by preparative HPLC chromatography (RP 18,acetonitrile, water, 0.01% TFA) to give 143 mg (50%) of the desiredproduct.

M+H⁺=436.

LC/MS retention time=1.784.

EXAMPLE 195 Preparation of3-[3-chloro-4-(propane-2-sulfonyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

40 mg (0.1 mmol) of3-(3-chloro-4-isopropylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionewere dissolved in 2 ml of methylene chloride and treated with a solutionof 37 mg (0.15 mmol) of m-chloroperbenzoic acid in 2 ml of methylenechloride. The reaction was monitored by TLC and stopped when thesulfoxide and the sulfone were formed in equal amounts. The mixture wasevaporated to dryness and purified by flash chromatography (SiO₂,methylene chloride/methanol=98/2) to give 4 mg of3-[3-chloro-4-(propane-2-sulfonyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dioneand 7 mg of3-[3-chloro-4-(propane-2-sulfinyl)phenyl]-5,5-dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4-dione.

M+H⁺=436.

LC/MS retention time=0.970.

EXAMPLE 196 Preparation of3-[3-chloro-4-(propane-2-sulfinyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dione

Prepared as described above.

M+H⁺=420.

LC/MS retention time=0.932.

2-(Isoquinolin-5-ylamino)-2-methylpropionitrile

5.0 g (34.7 mmol) of 5-aminoisoquinoline, 5.1 ml (69.4 mmol) of acetoneand 945 mg (6.94 mmol) of zinc chloride were dissolved in 100 ml ofacetonitrile and treated at 0° C. with 6.9 g (69.4 mmol) oftrimethylsilyl cyanide. The mixture was refluxed for 3 hours, thesolvent was then evaporated off and the residue was taken up in 200 mlof sodium hydrogen carbonate and extracted three times with ethylacetate. The combined organic phases were dried and the residueremaining after evaporation was purified by flash chromatography (SiO₂,methylene chloride/methanol=95/5) to give 6.0 g (82%) of the desiredproduct.

M+H⁺=212.

LC/MS retention time=0.696.

General Procedure 2 Synthesis of alkylsulfanylanilines

1.1 g (8 mmol) of 4-aminothiophenol and 896 mg (8 mmol) of potassiumtert-butoxide were dissolved in 10 ml of DMF and stirred for 45 minutesunder an argon atmosphere. Next, 8.8 mmol of the corresponding alkylbromide were added and the mixture was stirred for 3 hours at roomtemperature, poured into water and extracted with ethyl acetate. Thecombined organic phases were dried and evaporated. The residual productwas essentially pure and could be used without further purification.

4-(3-Methoxypropylsulfanyl)phenylamine

Prepared according to the general procedure 2.

M+H⁺=197.

LC/MS retention time=0.777.

4-Isopropylsulfanylphenylamine

Prepared according to the general procedure 2.

M+H⁺=266.

LC/MS retention time=0.173.

4-[3-(4-Methylpiperazin-1-yl)propylsulfanyl]phenylamine

Prepared according to the general procedure 2.

M+H⁺=168.

LC/MS retention time=0.894.

General Procedure 3 Preparation of3-(3-chloro-4-alkylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-diones

371 mg (2.3 mmol) of carbonyldiimidazole, 41 mg (0.5 mmol) of imidazoleand 1.9 mmol of the respective alkylsulfanylaniline were dissolved at 0°C. in 10 ml of THF and stirred for 1 hour. Next, 280 mg (1.35 mmol) ofmethyl 2-methyl-2-[(pyrid-4-yl-methyl)amino]propionate dissolved in 5 mlof THF were added and the mixture was refluxed for 5 hours. Next, thesolvent was evaporated off and the material remaining after evaporationwas purified by preparative HPLC chromatography (RP 18, acetonitrile,water, 0.01% TFA).

EXAMPLE 197 Preparation of5,5-dimethyl-3-(4-methylsulfanylphenyl)-1-pyrid-4-yl-methylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 3.

M+H⁺=342.

LC/MS retention time=0.942.

EXAMPLE 198 Preparation of3-[4-(3-methoxypropylsulfanyl)phenyl]-5,5-dimethyl-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 3.

M+H⁺=400.

LC/MS retention time=1.007.

EXAMPLE 199 Preparation of3-(4-isopropylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 3.

M+H⁺=370.

LC/MS retention time=1.096.

EXAMPLE 200 Preparation of5,5-dimethyl-3-{4-[3-(4-methylpiperazin-1-yl)propylsulfanyl]phenyl}-1-pyrid-4-ylmethylimidazolidine-2,4-dionetrifluoroacetate

Prepared according to the general procedure 3.

M+H⁺=468.

LC/MS retention time=0.689

EXAMPLE 2015,5-Dimethyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoro-methoxyphenyl)imidazolidine-2,4-dione

0.1 g of sodium hydride (at 60%) is added to a solution of 0.65 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione in 40ml of anhydrous THF, under an inert atmosphere of argon at a temperaturein the region of 20° C. Stirring is maintained at this temperature for30 minutes. 0.47 g of 4-chloromethyl-6-methoxyquinoline dissolved in 10ml of THF is added. The reaction medium is refluxed for 16 hours. Aftercooling, 100 ml of water and 75 ml of ethyl acetate are added. Afterseparation of the phases by settling, the organic phase is dried oversodium sulfate, filtered and then concentrated under reduced pressure.The brown oil obtained is purified by flash chromatography (SiO₂,EtOAc/cyclohexane, 50/50 by volume, as eluent, Ar). The fractionscontaining the product are concentrated under reduced pressure. 0.36 gof5,5-dimethyl-1-(6-methoxyquinolin-4-yl-methyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 3.96 (s:3H); 5.10 (broad s: 2H); 7.46 (dd, J=9 and 3 Hz: 1H); 7.54 (d, J=3 Hz:1H); 7.56 (broad d, J=9 Hz: 2H); 7.61 (d, J=4.5 Hz: 1H); 7.68 (broad d,J=9 Hz: 2H); 8.00 (d, J=9 Hz: 1H); 8.72 (d, J=4.5 Hz: 1H).

Mass IE m/z=459 M+. base peak

m/z=213 C₁₂H₉N₂O₂ ⁺

m/z=172 C₁₁H₁₀NO⁺

The compound5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione isprepared according to the process described in Example 63.

Preparation of 4-chloromethyl-6-methoxyquinoline

1.16 ml of triethylamine and 0.64 ml of methanesulfonyl chloride aresuccessively added to a solution of 1.2 g of4-hydroxymethyl-6-methoxyquinoline in 45 ml of dichloromethane, under aninert atmosphere of argon at a temperature in the region of 20° C.Stirring is maintained at this temperature for 3 hours. The reactionmedium is concentrated under reduced pressure to give a brown residue.The product is used without further purification in the following step.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 3.97 (s: 3H); 5.30 (s:2H); 7.48 (dd, J=9 and 3 Hz: 1H); 7.52 (d, J=3 Hz: 1H); 7.62 (d, J=4.5Hz: 1H); 8.00 (d, J=9 Hz: 1H); 8.75 (d, J=4.5 Hz: 1H).

Mass IE m/z=207 M⁺.

m/z=172 (M-Cl)⁺base peak

m/z=157 (m/z=172-CH₃)⁺

m/z=129 (m/z=157-CO)⁺

Preparation of 4-hydroxymethyl-6-methoxyquinoline

17 ml of a 1 M solution of LiAlH₄ in THF are added dropwise to asolution of 4 g of 4-ethoxycarbonyl-6-methoxyquinoline in 100 ml ofanhydrous THF, under an inert atmosphere of argon at a temperature inthe region of 5° C. The reaction medium is maintained with stirring for16 hours at a temperature in the region of 20° C. 50 ml of water and 50ml of ethyl acetate are added. After separation of the phases bysettling, the organic phase is dried over sodium sulfate, filtered andthen concentrated under reduced pressure. The foam obtained is purifiedby flash chromatography (SiO₂, EtOAc as eluent, Ar). The fractionscontaining the product are concentrated under reduced pressure. 0.86 gof 4-hydroxymethyl-6-methoxyquinoline is thus obtained, thecharacteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 3.93 (s: 3H); 5.02 (d,J=5.5 Hz: 2H); 5.57 (t, J=5.5 Hz: 1H); 7.30 (d, J=3 Hz: 1H); 7.38 (dd,J=9 and 3 Hz: 1H); 7.50 (d, J=4.5 Hz: 1H); 7.92 (d, J=9 Hz: 1H); 8.69(d, J=4.5 Hz: 1H).

Mass IE, m/z=189 M⁺. base peak

m/z=174 (M-CH₃)⁺

m/z=160 (M-CHO)⁺

m/z=146 (m/z=174-CO)⁺

m/z=117 (m/z=146-CHO)⁺.

EXAMPLE 2025,5-Dimethyl-1-(6-hydroxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

6 ml of a 1M solution of boron tribromide in CH₂Cl₂ are added to asolution of 0.26 g of5,5-dimethyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionein 40 ml of dichloromethane, under an inert atmosphere of argon at atemperature in the region of 0° C. The reaction medium is stirred at atemperature in the region of 20° C. for 16 hours. 5 ml of methanol areadded dropwise. After stirring for 30 minutes at this temperature, 50 mlof water, 30 ml of CH₂Cl₂ and 10 ml of saturated NaHCO₃ are added. Afterseparation of the phases by settling, the organic phase is dried oversodium sulfate, filtered and then concentrated under reduced pressure.The beige-colored foam obtained is purified by flash chromatography(SiO₂, EtOAc as eluent, Ar). The fractions containing the product areconcentrated under reduced pressure. 0.17 g of5,5-dimethyl-1-(6-hydroxyquinolin-4-yl-methyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.46 (s: 6H); 5.00(broad s: 2H); 7.30 to 7.40 (mt: 2H); 7.51 (d, J=4.5 Hz: 1H); 7.55(broad d, J=8.5 Hz: 2H); 7.69 (d, J=8.5 Hz: 2H); 7.94 (d, J=9 Hz: 1H);8.64 (d, J=4.5 Hz: 1H); 10.12 (unresolved complex: 1H).

Mass IE m/z=445 M⁺.

m/z=199 C₁₁H₇N₂O₂ ⁺

m/z=158 C₁₀H₈NO⁺ base peak

EXAMPLE 2035,5-Dimethyl—(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

The product is prepared according to the procedure described in Example59, starting with 0.94 g of methyl2-methyl-2-[(7-methoxyquinolin-4-ylmethyl)amino]propanoate instead ofmethyl 2-methyl-2-[(quinolin-4-ylmethyl)amino]propanoate used in Example59, and 1.7 g of 4-(trifluoromethoxyphenyl) isocyanate. Afterpurification by flash chromatography on a column (SiO₂,cyclohexane/ethyl acetate 70/30 by volume and then CH2Cl2/MeOH 90/10 byvolume as eluents, Ar), 1.45 g of the expected product are obtained.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 3.96 (s:3H); 5.12 (broad s: 2H); 7.35 (dd, J=9 and 3 Hz: 1H); 7.47 (d, J=3 Hz:1H); 7.49 (d, J=4.5 Hz: 1H); 7.55 (broad d, J=9 Hz: 2H); 7.68 (broad d,J=9 Hz: 2H); 8.19 (d, J=9 Hz: 1H); 8.80 (d, J=4.5 Hz: 1H).

Mass IE m/z=459 M⁺. base peak

m/z=444 (M-CH₃)⁺

m/z=213 C₁₂H₉N₂O₂ ⁺

m/z=172 C₁₁H₁₀NO⁺

Preparation of methyl 2-((7-methoxyquinolin-4-ylmethyl)amino)propanoate

A mixture of 1.23 g of methyl α-aminoisobutyrate hydrochloride and 1.12ml of triethylamine in 30 ml of dichloromethane is stirred at 0° C. for20 minutes. Next, 1 g of magnesium sulfate and 1.5 g of7-methoxyquinoline-4-carbaldehyde are added. Stirring is continued for15 hours at room temperature and the mixture is then concentrated underreduced pressure. The residue is taken up in 35 ml of methanol, thesolution obtained is cooled to 0° C. and 0.31 g of sodium borohydride isthen added portionwise. The reaction medium is stirred at a temperaturein the region of 20° C. for 15 hours. The reaction medium isconcentrated under reduced pressure. The residue obtained is taken up in100 ml of EtOAc. The precipitate formed is filtered off and the filtrateis concentrated under reduced pressure and then purified by flashchromatography on a column (SiO₂, EtOAc as eluent, Ar), and 0.95 g ofthe expected product is obtained.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.35 (s: 6H); 2.63 (t,J=7.5 Hz: 1H); 3.70 (s: 3H); 3.93 (s: 3H); 4.05 (d, J=7.5 Hz: 2H); 7.28(dd, J=9 and 3 Hz: 1H); 7.41 (d, J=3 Hz: 1H); 7.43 (d, J=4.5 Hz: 1H);8.12 (d, J=9 Hz: 1H); 8.76 (d, J=4.5 Hz: 1H).

Mass IC m/z=289 MH⁺ base peak

m/z=229 (M-C₂H₄O₂)⁺

Preparation of 7-methoxyquinoline-4-carbaldehyde

A mixture of 1.9 g of selenium oxide dissolved in 35 ml of dioxane isadded dropwise to a solution of 2.7 g of 4-methyl-7-methoxyquinoline in35 ml of dioxane preheated to 65° C. At the end of the addition, thebrown suspension is heated to a temperature in the region of 80° C. for5 hours. The reaction medium is stirred for 16 hours at a temperature inthe region of 20° C. The greenish suspension is suction-filtered andthen washed with EtOAc. The filtrate is concentrated under reducedpressure. The suspension obtained is crystallized from isopropyl etherto give 1.54 g of 7-methoxyquinoline-4-carbaldehyde.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 3.99 (s: 3H); 7.48(dd, J=9 and 3 Hz: 1H); 7.57 (d, J=3 Hz: 1H); 7.90 (d, J=4.5 Hz: 1H);8.89 (d, J=9 Hz: 1H); 9.19 (d, J=4.5 Hz: 1H); 10.52 (s: 1H).

Mass IC m/z=188 MH⁺ base peak

Preparation of 4-methyl-7-methoxyquinoline

4 g of triphenylphosphine, 5.3 g of lithium chloride, 14 ml oftetramethyltin and 2.1 g of bis(triphenylphosphine)palladium(II)chloride are added to a solution of 6 g of 4-bromo-7-methoxyquinoline in100 ml of DMF, under an inert atmosphere of argon at a temperature inthe region of 20° C. The reaction medium is heated at a temperature inthe region of 120° C. for 16 hours. After cooling, the insolublematerial is filtered off. The filtrate is concentrated under reducedpressure. The residue obtained is taken up in 300 ml of EtOAc and 300 mlof water. After separation of the phases by settling, the organic phaseis dried over magnesium sulfate, filtered and then concentrated underreduced pressure. The oil obtained is taken up in 300 ml of EtOAc and300 ml of water and then acidified with hydrochloric acid to pH 1. Theaqueous phase is basified with sodium hydroxide to pH 10 and thenextracted with 300 ml of EtOAc. After separation of the phases bysettling, the organic phase is dried over magnesium sulfate, filteredand then concentrated under reduced pressure to give 2.7 g of4-methyl-7-methoxyquinoline, the characteristics of which product are asfollows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 2.65 (s: 3H); 3.94 (s:3H); 7.23 (broad d, J=4.5 Hz: 1H); 7.28 (dd, J=9 and 3 Hz: 1H); 7.40 (d,J=3 Hz: 1H); 8.01 (d, J=9 Hz: 1H); 8.58 (d, J=4.5 Hz: 1H).

Mass IE m/z=173 M⁺. base peak

m/z=158 (M-CH₃)⁺

m/z=143 (M-CH₂O)⁺.

m/z=130 (m/z=158-CO)⁺

Preparation of 4-bromo-7-methoxyquinoline

22.74 g of 4-hydroxy-7-methoxyquinoline are added to 200 g of phosphorusoxybromide preheated to a temperature in the region of 110° C. Thereaction medium is heated at this same temperature for 3 hours. Thereaction medium is poured, while hot, into a mixture of 500 ml of EtOAcand 500 ml of ice-cold water. The medium is neutralized with potassiumcarbonate to pH 7. After separation of the phases by settling, theorganic phase is dried over magnesium sulfate, evaporated under reducedpressure and then purified by column chromatography (SiO₂,EtOAc/cyclohexane 50/50 by volume as eluents, Ar), and 14.6 g of theexpected product are obtained.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 3.97 (s: 3H); 7.43(dd, J=9 and 3 Hz: 1H); 7.49 (d, J=3 Hz: 1H); 7.79 (d, J=4.5 Hz: 1H);8.06 (d, J=9 Hz: 1H); 8.67 (d, J=4.5 Hz: 1H).

Mass IE m/z=237 M⁺. base peak

-   4-Hydroxy-7-methoxyquinoline is prepared according to the process    described in: J. Am. Chem. Soc., 68, 1268, 1946.

EXAMPLE 2045,5-Dimethyl-1-(7-hydroxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

A mixture of 0.89 g of5,5-dimethyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

and 5.5 g of pyridine hydrochloride is heated at a temperature in theregion of 220° C. for 4 hours. After cooling, 200 ml of water and 100 mlof CH₂Cl₂ are added. After separation of the phases by settling, theorganic phase is dried over sodium sulfate, filtered and thenconcentrated under reduced pressure. The solid obtained is purified byflash chromatography (SiO₂, EtOAc/CH₂Cl₂ 40/60 by volume as eluent, Ar).The fractions containing the product are concentrated under reducedpressure. 85 mg of5,5-dimethyl-1-(7-hydroxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneare thus obtained, the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 5.08(broad s: 2H); 7.24 (dd, J=9 and 3 Hz: 1H); 7.30 (d, J=3 Hz: 1H); 7.38(d, J=4.5 Hz: 1H); 7.55 (broad d, J=9 Hz: 2H); 7.68 (broad d, J=9 Hz:2H); 8.10 (d, J=9 Hz: 1H); 8.71 (d, J=4.5 Hz: 1H); from 9.90 to 10.50(broad unresolved complex: 1H).

Mass IE m/z=445 M⁺. base peak

m/z=430 (M-CH₃)⁺

m/z=199 C₁₁H₇N₂O₂ ⁺

m/z=158 C₁₀H₈NO⁺

EXAMPLE 2055,5-Dimethyl-1-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.44 g of tosyl chloride is added to a solution of 0.8 g of5,5-dimethyl-1-(N-oxyquinolin-4-yl-methyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionein 10 ml of chloroform, under an inert atmosphere of argon at atemperature in the region of 5° C. After stirring for 30 minutes at thissame temperature, 1.5 ml of 32% aqueous ammonia are added. Thetemperature is allowed to rise to 20° C. The reaction medium is stirredat a temperature in the region of 20° C. for 16 hours. 100 ml of waterare added. After separation of the phases by settling, the organic phaseis dried over sodium sulfate, filtered and then concentrated underreduced pressure. The solid obtained is purified by flash chromatography(SiO₂, EtOAc as eluent, Ar). The fractions containing the product areconcentrated under reduced pressure. 200 mg of5,5-dimethyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dioneare thus obtained, the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.49 (s: 6H); 4.96(broad s: 2H); 6.36 (broad s: 2H); 6.81 (s: 1H); 7.23 (mt: 1H); 7.51(mt: 2H); 7.58 (broad d, J=9 Hz: 2H); 7.68 (broad d, J=9 Hz: 2H); 7.91(d, J=8.5 Hz: 1H).

Mass IE m/z=444M⁺. base peak

m/z=429 (M-CH₃)⁺

m/z=198 C₁₁H₈N₃O⁺

m/z=158 C₁₀H₁₀N₂ ⁺

EXAMPLE 2065,5-Dimethyl-1-(N-oxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.78 g of m-chloroperbenzoic acid is added to a solution of 1.95 g of5,5-dimethyl-1-(quinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionein 200 ml of chloroform and 10 ml of methanol, under an inert atmosphereof argon, at a temperature in the region of 20° C. The reaction mediumis stirred at a temperature in the region of 20° C. for 4 hours. Afurther 0.8 g of m-chloroperbenzoic acid is added. The reaction mediumis concentrated under reduced pressure. The product is crystallized fromisopropyl ether to give 1.76 g of5,5-dimethyl-1-(N-oxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione,the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 5.09(broad s: 2H); 7.55 (broad d, J=8.5 Hz: 2H); 7.63 (d, J=4.5 Hz: 1H);7.68 (broad d, J=8.5 Hz: 2H); 7.85 (broad t, J=8.5 Hz: 1H); 7.91 (broadt, J=8.5 Hz: 1H); 8.35 (broad d, J=8.5 Hz: 1H); 8.56 (d, J=4.5 Hz: 1H);8.64 (broad d, J=8.5 Hz: 1H).

Mass ES m/z=446 MH⁺ base peak

EXAMPLE 2075,5-Dimethyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.17 ml of phosphorus oxychloride is added to a solution of 4 ml of DMFand 2 ml of toluene, under an inert atmosphere of argon at a temperaturein the region of 5° C. After stirring for 30 minutes at this sametemperature, 0.4 g of5,5-dimethyl-1-(N-oxyquinolin-4-yl-methyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dionein 10 ml of toluene is added. The reaction medium is stirred at atemperature in the region of 5° C. for 2 and a half hours. Thetemperature is allowed to return to 20° C. The reaction medium isconcentrated under reduced pressure. The residue obtained is taken up in50 ml of EtOAc and washed with saturated NaHCO₃ solution. Afterseparation of the phases by settling, the organic phase is dried oversodium sulfate, filtered and then concentrated under reduced pressure.The product is crystallized from isopropyl ether to give 0.37 g of5,5-dimethyl-1-(2-chloroquinolin-4-yl-methyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione,the characteristics of which product are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.50 (s: 6H); 5.17(broad s: 2H); 7.56 (broad d, J=8.5 Hz: 2H); 7.71 (broad d, J=8.5 Hz:2H); 7.76 (s: 1H); 7.76 (split t, J=8 and 1.5 Hz: 1H); 7.89 (split t,J=8 and 1.5 Hz: 1H); 8.03 (broad d, J=8 Hz: 1H); 8.31 (broad d, J=8 Hz:1H).

Mass IE m/z=463 M⁺. base peak

m/z=448 (M-CH₃)⁺

m/z=428 (M-Cl)⁺

m/z=358 (m/z=428-C₄H₆O)⁺

m/z=217 C₁₁H₆N₂OCl⁺

m/z=176 C₁₀H₇NCl⁺

EXAMPLE 2085,5-Dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.028 g of sodium hydride is added to a solution of 0.1 g of5,5-dimethyl-3-(4-trifluoro-methoxyphenyl)imidazolidine-2,4-dione in 2ml of anhydrous dimethylformamide, under an inert atmosphere of argon ata temperature in the region of 20° C. Stirring is continued at thistemperature for 30 minutes. A solution of 0.1 g of2-chloro-4-(bromomethyl)pyridine in 2 ml of dimethylformamide is added,followed by addition of ice-cold water after reaction for 10 minutes.The reaction medium is placed on a cartridge 20 mm in diameter packedwith 17 g of octadecyl-grafted 50 μm silica conditioned successivelywith acetonitrile and then with water. The elution is performed bygradient using the mixture (water/acetonitrile) of from 0 to 100%acetonitrile. The fractions containing the expected product areconcentrated under reduced pressure. 0.130 g of crude product is thusobtained, which product is purified by a double chromatography using acartridge packed with 10 g of 20-40 μm of conditioned silica, and theneluted with a mixture (cyclohexane/ethyl acetate), (8/2)(v/v) at a flowrate of 5 ml/minute. The fractions between 30 and 75 ml are concentratedunder reduced pressure. 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white powder, the characteristics ofwhich product are as follows:

-   m.p. 134° C.

Mass IE m/z=413 M⁺. base peak

m/z=398 (M-CH₃)⁺

m/z=203 C₈H₄NO₂F₃ ⁺.

m/z=167 C₇H₄N₂OCl⁺

m/z=126 C₆H₅NCl⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 4.67 (s:2H); 7.50 (broad d, J=5.5 Hz: 1H); 7.54 (broad d, J=9 Hz: 2H); 7.61(broad s: 1H); 7.66 (broad d, J=9 Hz: 2H); 8.40 (d, J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione isdescribed in Example 63.

EXAMPLE 2095,5-Dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.015 g of sodium hydride is added to a solution of 0.175 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione in 2 mlof anhydrous dimethylformamide, under an inert atmosphere of argon at atemperature in the region of 20° C. Stirring is maintained at thistemperature for 30 minutes. A solution of 0.185 g of2-ethoxy-4-(bromomethyl)pyridine in 2 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 10minutes. The reaction mixture is placed on a cartridge 37 mm in diameterpacked with 65 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenwith the mixture (water/acetonitrile)(95/5) (v/v). The elution isperformed with a mixture (water/acetonitrile)(95/5)(v/v) over 20minutes, followed by a linear gradient of from 5% to 95% acetonitrileover 60 minutes, at a flow rate of 10 ml/minute. The fractions between700 and 760 ml are concentrated under reduced pressure. 0.145 g of5,5-dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE m/z=423 M⁺.

m/z=408 (M-CH₃)⁺ base peak

m/z=395 (M-C₂H₄)⁺.

m/z=203 C₈H₄NO₂F₃ ⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.32 (t, J=7 Hz: 3H);1.42 (s: 6H); 4.30 (q, J=7 Hz: 2H); 4.58 (broad s: 2H); 6.85 (broad s:1H); 7.01 (broad d, J=5.5 Hz: 1H); 7.52 (broad d, J=8.5 Hz: 2H); 7.63(broad d, J=8.5 Hz: 2H); 8.10 (d, J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione isdescribed in Example 63.

EXAMPLE 2105,5-Dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.009 g of sodium hydride is added to a solution of 0.064 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione in 1 mlof anhydrous dimethylformamide, under an inert atmosphere of argon, at atemperature in the region of 20° C. Stirring is continued at thistemperature for 30 minutes. A solution of 0.062 g of2-ethyl-4-(bromomethyl)pyridine in 0.5 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 10minutes. The reaction mixture is placed on a cartridge 27 mm in diameterpacked with 25 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenwith the mixture (water/acetonitrile)(95/5)(v/v). The elution isperformed with a mixture (water/acetonitrile) (95/5)(v/v) over 20minutes, followed by a linear gradient of from 5% to 95% acetonitrileover 60 minutes, at a flow rate of 10 ml/minute. The fractions between750 and 790 ml are concentrated under reduced pressure. 0.06 g of5,5-dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE m/z=407 M⁺. base peak

m/z=392 (M-CH₃)⁺

m/z=203 C₈H₄NO₂F₃ ⁺.

m/z=120 C₈H₁₀N⁺

¹H NMR spectrum (400 MHz, (CD₃)₂SO d6, δ in ppm): 1.27 (t, J=7.5 Hz:3H); 1.44 (s: 6H); 2.75 (q, J=7.5 Hz: 2H); 4.54 (s: 2H); 7.10 (broad d,J=5.5 Hz: 1H); 7.15 (broad s: 1H); 7.39 (broad d, J=8.5 Hz: 2H); 7.49(d, J=8.5 Hz: 2H); 8.26 (d, J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethoxy-phenyl)imidazolidine-2,4-dione isdescribed in Example 63.

EXAMPLE 2115,5-Dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanyl-phenyl)imidazolidine-2,4-dione

0.046 g of sodium hydride is added to a solution of 0.175 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 3 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon, at a temperature in the region of 20° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.166 g of2-chloro-4-(bromomethyl)pyridine in 2 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 10minutes. The reaction mixture is placed on a cartridge 37 mm in diameterpacked with 65 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenwith the mixture (water/acetonitrile)(95/5)(v/v). The elution isperformed with a mixture (water/acetonitrile)(95/5)(v/v) over 20minutes, followed by a linear gradient of from 5 to 95% acetonitrileover 60 minutes, at a flow rate of 10 ml/minute. The fractions between740 and 780 ml are concentrated under reduced pressure. 0.03 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white powder, the characteristics ofwhich product are as follows:

-   m.p. 111° C.

Mass IC

m/z=447 MNH₄ ⁺

m/z=430 MH⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 4.67(broad s: 2H); 7.49 (broad d, J=5.5 Hz: 1H); 7.61 (broad s: 1H); 7.70(broad d, J=8.5 Hz: 2H); 7.88 (broad d, J=8.5 Hz: 2H); 8.38 (d, J=5.5Hz: 1H).

Preparation of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

5.12 ml of triethylamine and 2.8 g of methyl α-aminoisobutyratehydrochloride are added to a solution of 4 g of4-trifluoromethylsulfanylphenyl isocyanate in 40 ml of toluene, under aninert atmosphere of argon at a temperature in the region of 20° C. Themixture thus obtained is refluxed for 24 hours and then cooled to atemperature in the region of 20° C. The reaction mixture is concentratedto dryness under reduced pressure and the residue obtained is taken upin ethyl ether and filtered. 5.3 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)-imidazolidine-2,4-dioneare thus obtained, the characteristics of which product are as follows:

Mass IC

m/z=322 MNH₄ ⁺

m/z=102 triethylamineH⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 7.62(broad d, J=8.5 Hz: 2H); 7.85 (broad d, J=8.5 Hz: 2H); 8.72 (unresolvedcomplex: 1H).

The insoluble material thus obtained is taken up in dichloromethane andthen washed with water. 2.76 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneare thus obtained, which product is used for the subsequent synthesis.

EXAMPLE 2125,5-Dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.049 g of sodium hydride is added to a solution of 0.185 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 3.2 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 20° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.184 g of2-ethoxy-4-(bromomethyl)pyridine in 2 ml of dimethylformamide is added,followed by addition of ice-cold water after reaction for 10 minutes.The reaction mixture is placed on a cartridge 37 mm in diameter packedwith 65 g of octadecyl-grafted 40-60 μm silica conditioned successivelywith the mixture (water/acetonitrile)(5/95)(v/v) and then the mixture(water/acetonitrile) (95/5)(v/v). The elution was performed with amixture (water/acetonitrile)(95/5)(v/v) over 20 minutes, followed by alinear gradient of from 5% to 95% of acetonitrile over 60 minutes, at aflow rate of 10 ml/minute. The fractions between 520 and 700 ml areconcentrated under reduced pressure. The residue thus obtained ispurified by flash chromatography using a cartridge packed with 2 g ofconditioned 15-35 μm silica, and then eluted with a mixture(cyclohexane/ethyl acetate)(9/1)(v/v). The fractions containing theexpected product are concentrated under reduced pressure. 0.01 g of5,5-dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE

m/z=439 M⁺.

m/z=424 (M-CH₃)⁺ base peak

m/z=411 (M-C₂H₄)⁺.

m/z=219 C₈H₄NOSF₃ ⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.32 (t, J=7 Hz: 3H);1.42 (s: 6H); 4.30 (q, J=7 Hz: 2H); 4.58 (broad s: 2H); 6.86 (broad s:1H); 7.01 (broad d, J=5.5 Hz: 1H); 7.69 (broad d, J=8.5 Hz: 2H); 7.88(broad d, J=8.5 Hz: 2H); 8.10 (broad d, J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionej s described in Example 211.

EXAMPLE 2135,5-Dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.021 g of sodium hydride is added to a solution of 0.135 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 2 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 20° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.126 g of2-ethyl-4-(bromomethyl)pyridine in 1 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 10minutes. The reaction mixture is placed on a cartridge 37 mm in diameterpacked with 65 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenthe mixture (water/acetonitrile)(95/5)(v/v). The elution was performedwith a mixture (water/acetonitrile)(95/5)(v/v) over 20 minutes, followedby a linear gradient of from 5% to 95% of acetonitrile over 60 minutesand by an elution with 100% acetonitrile for 10 minutes, at a flow rateof 10 ml/minute. The fractions between 800 and 880 ml are concentratedunder reduced pressure. 0.120 g of5,5-dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE

m/z=423 M⁺. base peak

m/z=408 (M-CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=120 C₈H₁₀N⁺

¹H NMR spectrum (400 MHz, (CD₃)₂SO d6, δ in ppm): 1.23 (t, J=7.5 Hz:3H); 1.42 (s: 6H); 2.75 (q, J=7.5 Hz: 2H); 4.62 (broad s: 2H); 7.25(broad d, J=5.5 Hz: 1H); 7.30 (broad s: 1H); 7.70 (d, J=8.5 Hz: 2H);7.88 (d, J=8.5 Hz: 2H); 8.43 (d, J=5.5 Hz: 1H). The compound5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis described iii Example 211.

EXAMPLE 2145,5-Dimethyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.023 g of sodium hydride is added to a solution of 0.081 g of5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione in 2 mlof anhydrous dimethylformamide, under an inert atmosphere of argon at atemperature in the region of 20° C. Stirring is continued at thistemperature for 35 minutes. A solution of 0.071 g of2-bromo-4-(bromomethyl)pyridine in 1 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 15minutes. The reaction mixture is placed on a cartridge 16 mm in diameterpacked with 5 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenthe mixture (water/acetonitrile)(95/5)(v/v). The elution was performedwith a linear gradient of from 5% to 95% of acetonitrile over 30 minutesthen with a mixture (water/acetonitrile)(5/95)(v/v) over 10 minutes, ata flow rate of 5 ml/minute. The fractions between 90 and 100 ml areconcentrated under reduced pressure. 0.015 g of5,5-dimethyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of a white foam, the characteristics ofwhich product are as follows:

Mass IE

m/z=457 M⁺. base peak

m/z=442 (M-CH₃)⁺

m/z=211 C₇H₄N₂OBr⁺

m/z=203 C₈H₄NO₂F₃ ⁺.

m/z=170 C₆H₅Br⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 4.67(broad s: 2H); 7.52 (broad d, J=5.5 Hz: 1H); 7.54 (broad d, J=9 Hz: 2H);7.66 (broad d, J=9 Hz: 2H); 7.75 (broad s: 1H); 8.37 (d, J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione isdescribed in Example 63.

EXAMPLE 2155,5-Dimethyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.025 g of sodium hydride is added to a solution of 0.096 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 2 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 20° C. Stirring is continued atthis temperature for 25 minutes. A solution of 0.060 g of2-fluoro-4-(bromomethyl)pyridine in 1 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 15minutes. The reaction mixture is placed on a cartridge 16 mm in diameterpacked with 5 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenthe mixture (water/acetonitrile)(95/5)(v/v). The elution was performedwith a linear gradient of from 5% to 95% of acetonitrile over 30 minutesthen with a mixture (water/acetonitrile (5/95) (v/v) over 10 minutes, ata flow rate of 5 ml/minute. The fractions between 105 and 125 ml areconcentrated under reduced pressure. 0.069 g of5,5-dimethyl-1-(2-fluoropyrid-4-yl-methyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white solid, the characteristics ofwhich are as follows:

-   m.p.: 82° C.

Mass IE

m/z=413 M⁺. base peak

m/z=398 (M-CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=151 C₇H₄N₂OF⁺

m/z=110 C₆H₅NF⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 4.72(broad s: 2H); 7.29 (broad s: 1H); 7.43 (broad d, J=5.5 Hz: 1H); 7.71(broad d, J=8.5 Hz: 2H); 7.89 (broad d, J=8.5 Hz: 2H); 8.23 (d, J=5.5Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis described in Example 211.

EXAMPLE 2165,5-Dimethyl-1-(2-cyanopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.037 g of sodium hydride is added to a solution of 0.139 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 4 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 20° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.090 g of2-cyano-4-(bromomethyl)pyridine in 1 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 15minutes. The reaction mixture is placed on a cartridge 20 mm in diameterpacked with 10 g of octadecyl-grafted 40-60 μm silica conditionedsuccessively with the mixture (water/acetonitrile)(5/95)(v/v) and thenthe mixture (water/acetonitrile)(95/5)(v/v). The elution was performedwith a linear gradient of from 5% to 95% of acetonitrile over 30 minutesthen with a mixture (water-acetonitrle)(5/95) (v/v) over 10 minutes, ata flow rate of 5 ml/minute. The fractions between 210 and 230 ml areconcentrated under reduced pressure. 0.1 g of5,5-dimethyl-1-(2-cyanopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a solid, the characteristics of whichare as follows:

-   m.p.: 148° C.

Mass IE

m/z=420 M⁺. base peak

m/z=405 (M-CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=158 C₈H₄N₃O⁺

m/z=117 C₇H₅N₂ ⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 4.74(broad s: 2H); 7.72 (broad d, J=9 Hz: 2H); 7.81 (dd, J=5.5 and 2 Hz:1H); 7.89 (broad d, J=9 Hz: 2H); 8.15 (broad s: 1H); 8.72 (broad d,J=5.5 Hz: 1H).

The compound5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis described in Example 211.

EXAMPLE 2175,5-Dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A solution of 0.09 g of5,5-dimethyl-1-(2-cyanopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 5 ml of 5N hydrochloric acid is refluxed for about 16 hours. Thereaction mixture is concentrated under reduced pressure and the crudeproduct thus obtained is purified by flash chromatography using acartridge 20 mm in diameter packed with 10 g of conditioned 20-40 μmsilica, and then eluted with a mixture(dichloromethane/methanol)(9/1)(v/v) at a flow rate of 8 ml/minute. Thefractions between 40 and 200 ml are concentrated under reduced pressure.0.06 g of5,5-dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE

m/z=439 M⁺.

m/z=395 (M-CONH₂)⁺ base peak

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=185 C₇H₉N₂O₂S⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 4.76(broad s: 2H); 7.70 (d, J=8.5 Hz: 2H); 7.72 (mt: 1H); 7.89 (d, J=8.5 Hz:2H); 8.12 (broad s: 1H); 8.68 (d, J=5.5 Hz: 1H).

EXAMPLE 2185,5-Dimethyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.025 g of methylamine hydrochloride, 0.005 g of hydroxybenzotriazolehydrate, 0.105 ml of triethylamine and 72 mg of1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride aresuccessively added to a solution of 0.055 g of5,5-dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 2 ml of dichloromethane, under an inert atmosphere of argon, at atemperature in the region of 20° C. Stirring is continued at thistemperature for about 16 hours. The reaction mixture is washed withwater and the organic phase is dried over magnesium sulfate, filteredand then concentrated under reduced pressure. The crude product thusobtained is purified by flash chromatography using a cartridge 16 mm indiameter packed with 5 g of conditioned 20-40 μm silica, and then elutedwith a mixture (dichloromethane/methanol)(95/05)(v/v) at a flow rate of10 ml/minute. The fractions containing the expected product areconcentrated under reduced pressure. 0.013 g of5,5-dimethyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white powder, the characteristics ofwhich are as follows:

Mass IE

m/z=452 M⁺.

m/z=395 (M-C₂H₃₀N)⁺ base peak

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=148 C₈H₈N₂O⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 2.85 (d,J=5 Hz: 3H); 4.76 (broad s: 2H); 7.67 (dd, J=5 and 2 Hz: 1H); 7.70(broad d, J=8.5 Hz: 2H); 7.89 (broad d, J=8.5 Hz: 2H); 8.10 (broad s:1H); 8.60 (d, J=5 Hz: 1H); 8.75 (broad q, J=5 Hz: 1H).

EXAMPLE 2195,5-Dimethyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A solution of 0.04 g of5,5-dimethyl-1-(2-cyanopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 1 ml of 98% sulfuric acid is maintained at 40° C. for 30 minutes. Themixture is taken up in 15 ml of ice-cold water and then neutralized withnormal sodium hydroxide solution. The solution thus obtained isextracted with 100 ml of ethyl acetate. The organic phase is dried overmagnesium sulfate, filtered and then concentrated under reducedpressure. The crude product thus obtained is purified by flashchromatography using a cartridge 16 mm in diameter packed with 5 g ofconditioned 20-40 μm silica, and then eluted with dichloromethane at aflow rate of 10 ml/minute. The fractions containing the expected productare concentrated under reduced pressure. 0.017 g of5,5-dimethyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of an amorphous white powder, thecharacteristics of which product are as follows:

Mass IE

m/z=438 M⁺. base peak

m/z=423 (M-CH₃)⁺

m/z=393 (M-CH₃NO)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=135 C₇H₇N₂O⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 4.76(broad s: 2H); from 7.60 to 7.70 (mt: 2H); 7.71 (broad d, J=8.5 Hz: 2H);7.89 (broad d, J=8.5 Hz: 2H); 8.11 (broad s: 2H); 8.60 (d, J=5.5 Hz:1H).

EXAMPLE 2205,5-Dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.05 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione,0.5 ml of dimethylformamide, 0.034 g of potassium carbonate and 0.021 mlof morpholine is placed in a Personal Chemistry Emrys Optimisermicrowave oven. The mixture is irradiated with magnetic stirring at 210°C. for about 50 minutes. The reaction mixture is placed on a Bond ElutVarian cartridge of reference 1225-6053 containing 2 g of SCX phaseconditioned with dimethylformamide. The cartridge is washed withmethanol and then eluted with 2M ammoniacal methanol. The ammoniacalfractions are concentrated to dryness under reduced pressure. Theresidue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with a mixture (cyclohexane/ethylacetate)(8/2)(v/v) at a flow rate of 10 ml/minute. The fractions between160 and 260 ml are concentrated to dryness under reduced pressure. 0.01g of5,5-dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichproduct are as follows:

Mass IE

m/z=464 M⁺.

m/z=433 (M-CH₃O)⁺ base peak

m/z=419 (M-C₂H₅O)⁺

m/z=407 (M-C₃H₅O)⁺

m/z=379 (M-C₄H₅NO)⁺

m/z=203 C₈H₄NO₂F₃ ⁺.

m/z=176 C₁₀H₁₂N₂O⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 3.44(broad t, J=5 Hz: 4H); 3.72 (broad t, J=5 Hz: 4H); 4.53 (broad s: 2H);6.75 (broad d, J=5.5 Hz: 1H); 6.85 (broad s: 1H); 7.54 (broad d, J=8.5Hz: 2H); 7.64 (d, J=8.5 Hz: 2H); 8.10 (d, J=5.5 Hz: 1H).

EXAMPLE 2215,5-Dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.05 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneand 0.5 ml of morpholine is placed in a Personal Chemistry EmrysOptimiser microwave oven. The mixture is irradiated with magneticstirring at 160° C. for about 70 minutes. The reaction mixture ispurified by preparative LC/MS. The fractions containing the expectedproduct are concentrated to dryness under reduced pressure. The residuethus obtained is taken up in methanol and then placed on a Bond ElutVarian cartridge of reference 1225-6053 containing 2 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. 0.03 g of5,5-dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichare as follows:

Mass IE

m/z=480 M⁺.

m/z=449 (M-CH₃O)⁺ base peak

m/z=435 (M-C₂H₅O)⁺

m/z=423 (M-C₃H₅O)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=176 C₁₀H₁₂N₂O⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 3.45(broad t, J=5 Hz: 4H); 3.71 (broad t, J=5 Hz: 4H); 4.54 (broad s: 2H);6.75 (broad d, J=5.5 Hz: 1H); 6.84 (broad s: 1H); 7.68 (broad d, J=8.5Hz: 2H); 7.88 (d, J=8.5 Hz: 2H); 8.09 (d, J=5.5 Hz: 1H).

EXAMPLE 2225,5-Dimethyl-1-(2-dimethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.05 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.4 ml of isopropylamine and 0.1 ml of dimethylformamide is placed in aPersonal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 140° C. for about 130 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6053containing 2 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.0.013 g of5,5-dimethyl-1-(2-dimethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichare as follows:

Mass IC

m/z=439 MH⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 3.03 (s:6H); 4.53 (broad s: 2H); 6.62 (broad d, J=5.5 Hz: 1H); 6.65 (broad s:1H); 7.68 (broad d, J=8.5 Hz: 2H); 7.87 (d, J=8.5 Hz: 2H); 8.03 (d,J=5.5 Hz: 1H).

EXAMPLE 2235,5-Dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.5 ml of N-methyl-2-pyrrolidone, 0.016 mg of methylamine hydrochlorideand 0.064 ml of triethylamine is placed in a Personal Chemistry EmrysOptimiser microwave oven. The mixture is irradiated with magneticstirring at 180° C. for about 80 minutes. The reaction mixture ispurified by preparative LC/MS. The fractions containing the expectedproduct are concentrated to dryness under reduced pressure. The residuethus obtained is taken up in methanol and then placed on a Bond ElutVarian cartridge of reference 1225-6054 containing 3 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. The residue thusobtained is purified by flash chromatography using a cartridge 16 mm indiameter packed with 2 g of conditioned 15-35 μm silica, and then elutedwith dichloromethane, at a flow rate of 5 ml/minute. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. 0.021 g of5,5-dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous white powder, thecharacteristics of which product are as follows:

Mass IE

m/z=424 M⁺. base peak

m/z=396 (M-CH₂N)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=120 C₇H₈N₂ ⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 2.77 (d,J=5 Hz: 3H); 4.48 (broad s: 2H); 6.42 (mt: 1H); 6.46 (broad s: 1H); 6.52(broad d, J=5.5 Hz: 1H); 7.69 (broad d, J=8.5 Hz: 2H); 7.89 (broad d,J=8.5 Hz: 2H); 7.94 (d, J=5.5 Hz: 1H).

EXAMPLE 2245,5-Dimethyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of cyclohexylamine is placedin a Personal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 50 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6054containing 3 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 15 and 45 ml are concentrated todryness under reduced pressure. 0.017 g of5,5-dimethyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=492 M⁺.

m/z=449 (M-C₃H₇)⁺

m/z=435 (M-C₃H₇)⁺

m/z=410 (M-C₆H₁₀)⁺. base peak

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=175 C₁₁H₁₅N₂ ⁺

m/z=98 C₆H₁₂N⁺

¹H NMR spectrum (400 MHz, (CD₃)₂SO d6, δ in ppm): from 1.10 to 1.40 (mt:5H); 1.43 (s: 6H); from 1.55 to 2.00 (mt: 5H); 3.67 (mt: 1H); 4.45 (s:2H); 6.28 (d, J=8 Hz: 1H); 6.44 (broad s: 1H); 6.46 (broad d, J=5.5 Hz:1H); 7.68 (broad d, J=9 Hz: 2H); from 7.85 to 7.95 (mt: 3H).

EXAMPLE 2255,5-Dimethyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of isopropylamine is placedin a Personal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 70 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 10 and 35 ml are concentrated todryness under reduced pressure. 0.008 g of5,5-dimethyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=452 M⁺.

m/z=437 (M-CH₃)⁺ base peak

m/z=410 (M-C₃H₆)⁺.

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=134 C₈H₁₀N₂ ⁺.

m/z=58 C₃H₈N⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.13 (d, J=6.5 Hz:6H); 1.42 (s: 6H); 3.98 (mt: 1H); 4.45 (broad s: 2H); 6.27 (broad d,J=7.5 Hz: 1H); 6.42 (broad s: 1H); 6.46 (broad d, J=5.5 Hz: 1H); 7.68(broad d, J=8 Hz: 2H); 7.88 (broad d, J=8 Hz: 2H); 7.90 (d, J=5.5 Hz:1H).

EXAMPLE 2265,5-Dimethyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of piperidine is placed in aPersonal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 30 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 10 and 30 ml are concentrated todryness under reduced pressure. 0.07 g of5,5-dimethyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=478 M⁺. base peak

m/z=449 (M-C₂H₅)⁺

m/z=422 (M-C₄H₈)⁺.

m/z=395 (M-C₅H₉N)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=161 C₁₀H₁₃N₂ ⁺

m/z=84 C₅H₁₀N⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); from1.45 to 1.65 (mt: 6H); 3.52 (broad t, J=5 Hz: 4H); 4.52 (broad s: 2H);6.64 (broad d, J=5.5 Hz: 1H); 6.83 (broad s: 1H); 7.68 (d, J=8.5 Hz:2H); 7.88 (d, J=8.5 Hz: 2H); 8.04 (d, J=5.5 Hz: 1H).

EXAMPLE 2275,5-Dimethyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of N-methylpiperazine isplaced in a Personal Chemistry Emrys Optimiser microwave oven. Themixture is irradiated with magnetic stirring at 200° C. for about 30minutes. The reaction mixture is purified by preparative LC/MS. Thefractions containing the expected product are concentrated to drynessunder reduced pressure. The residue thus obtained is taken up inmethanol and then placed on a Bond Elut Varian cartridge of reference1225-6027 containing 5 g of SCX phase conditioned with methanol. Thecartridge is washed with methanol and then eluted with 2M ammoniacalmethanol. The ammoniacal fractions are concentrated to dryness underreduced pressure. The residue thus obtained is purified by flashchromatography using a cartridge 16 mm in diameter packed with 2 g ofconditioned 15-35 μm silica, and then eluted with dichloromethane, at aflow rate of 5 ml/minute. The fractions between 105 and 135 ml areconcentrated to dryness under reduced pressure. 0.028 g of5,5-dimethyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=493 M⁺.

m/z=423 (M-C₄H₈N)⁺. base peak

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=176 C₁₀H₁₄N₃ ⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 2.23 (s:3H); 2.40 (broad t, J=5 Hz: 4H); 3.50 (broad t, J=5 Hz: 4H); 4.53 (broads: 2H); 6.70 (broad d, J=5.5 Hz: 1H); 6.85 (broad s: 1H); 7.69 (d, J=8.5Hz: 2H); 7.88 (d, J=8.5 Hz: 2H); 8.07 (d, J=5.5 Hz: 1H).

EXAMPLE 2285,5-Dimethyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of aniline is placed in aPersonal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 30 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 40 and 85 ml are concentrated todryness under reduced pressure. 0.082 g of5,5-dimethyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=486 M⁺.

m/z=485 (M−H)⁺ base peak

m/z=417 (M-CF₃)⁺

m/z=182 C₁₂H₁₀N₂ ⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.46 (s: 6H); 4.55(broad s: 2H); 6.80 (broad d, J=5.5 Hz: 1H); 6.84 (broad s: 1H); 6.88(broad t, J=7.5 Hz: 1H); 7.25 (dd, J=8 and 7.5 Hz: 2H); 7.67 (broad d,J=8 Hz: 2H); 7.69 (d, J=8.5 Hz: 2H); 7.88 (broad d, J=8.5 Hz: 2H); 8.01(d, J=5.5 Hz: 1H); 9.01 (broad s: 1H).

EXAMPLE 2295,5-Dimethyl-1-[2-(4-piperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.6 ml of N-methyl-2-pyrrolidone and 0.123 g of piperazine is placed ina Personal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 30 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 45 and 110 ml are concentrated todryness under reduced pressure. 0.042 g of5,5-dimethyl-1-[2-(4-piperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IC

m/z=480 MH⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 2.79(broad t, J=5 Hz: 4H); 3.41 (broad t, J=5 Hz: 4H); 4.52 (broad s: 2H);6.69 (broad d, J=5.5 Hz: 1H); 6.82 (broad s: 1H); 7.69 (broad d, J=8.5Hz: 2H); 7.88 (d, J=8.5 Hz: 2H); 8.06 (d, J=5.5 Hz: 1H).

EXAMPLE 2305,5-Dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.5 ml of N-methyl-2-pyrrolidone, 0.019 g of ethylamine hydrochlorideand 0.064 ml of triethylamine is placed in a Personal Chemistry EmrysOptimiser microwave oven. The mixture is irradiated with magneticstirring at 200° C. for about 120 minutes. The reaction mixture ispurified by preparative LC/MS. The fractions containing the expectedproduct are concentrated to dryness under reduced pressure. The residuethus obtained is taken up in methanol and then placed on a Bond ElutVarian cartridge of reference 1225-6027 containing 5 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. The residue thusobtained is purified by flash chromatography using a cartridge 16 mm indiameter packed with 2 g of conditioned 15-35 μm silica, and then elutedwith dichloromethane, at a flow rate of 5 ml/minute. The fractionsbetween 280 and 300 ml are concentrated to dryness under reducedpressure. 0.033 g of5,5-dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

-   m.p.=136° C.

Mass IE

m/z=438M⁺.

m/z=423 (M-CH₃)⁺ base peak

m/z=395 (M-C₂H₅N)⁺

m/z=369 (M-CF₃)⁺

m/z=121 C₇H₉N₂ ⁺.

m/z=44 C₂H₆N⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.14 (t, J=7 Hz: 3H);1.44 (s: 6H); 3.26 (mt: 2H); 4.47 (broad s: 2H); 6.40 (broad t, J=5.5Hz: 1H); 6.45 (broad s: 1H); 6.50 (broad d, J=5.5 Hz: 1H); 7.69 (broadd, J=8.5 Hz: 2H); 7.89 (broad d, J=8.5 Hz: 2H); 7.92 (d, J=5.5 Hz: 1H).

EXAMPLE 2315,5-Dimethyl-1-(2-benzylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of benzylamine is placed ina Personal Chemistry Emrys Optimiser microwave oven. The mixture isirradiated with magnetic stirring at 200° C. for about 30 minutes. Thereaction mixture is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.The residue thus obtained is purified by flash chromatography using acartridge 16 mm in diameter packed with 2 g of conditioned 15-35 μmsilica, and then eluted with dichloromethane, at a flow rate of 5ml/minute. The fractions between 10 and 50 ml are concentrated todryness under reduced pressure. 0.035 g of5,5-dimethyl-1-(2-benzylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which are as follows:

-   m.p. 144° C.

Mass IE

m/z=500 M⁺. base peak

m/z=431 (M-—CF₃)⁺

m/z=196 C₁₃H₁₂N₂ ⁺.

m/z=106 C₇H₈N⁺

m/z=91 C₇H₇ ⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.39 (s: 6H); 4.47(broad s: 2H); 4.48 (d, J=6 Hz: 2H); 6.51 (broad s: 1H); 6.54 (broad d,J=5.5 Hz: 1H); 7.02 (broad t, J=6 Hz: 1H); from 7.15 to 7.35 (mt: 5H);7.68 (broad d, J=8.5 Hz: 2H); 7.89 (d, J=8.5 Hz: 2H); 7.92 (d, J=5.5 Hz:1H).

EXAMPLE 2325,5-Dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of para-methoxybenzylamineis placed in a Personal Chemistry Emrys Optimiser microwave oven. Themixture is irradiated with magnetic stirring at 200° C. for about 30minutes. The reaction mixture is purified by preparative LC/MS. Thefractions containing the expected product are concentrated to drynessunder reduced pressure. The residue thus obtained is taken up inmethanol and then placed on a Bond Elut Varian cartridge of reference1225-6027 containing 5 g of SCX phase conditioned with methanol. Thecartridge is washed with methanol and then eluted with 2M ammoniacalmethanol. The ammoniacal fractions are concentrated to dryness underreduced pressure. The residue thus obtained is purified by flashchromatography using a cartridge 16 mm in diameter packed with 2 g ofconditioned 15-35 μm silica, and then eluted with dichloromethane, at aflow rate of 5 ml/minute. The fractions between 5 and 55 ml areconcentrated to dryness under reduced pressure. 0.035 g of5,5-dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous powder, the characteristicsof which product are as follows:

Mass IE

m/z=530 M⁺.

m/z=461 (M-—CF₃)⁺

m/z=136 C₈H₁₀NO⁺

m/z=121 C₈HgO⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.39 (s: 6H); 3.72 (s:3H); 4.39 (d, J=5.5 Hz: 2H); 4.46 (broad s: 2H); 6.48 (broad s: 1H);6.53 (broad d, J=5.5 Hz: 1H); 6.87 (broad d, J=8.5 Hz: 2H); 6.93 (t,J=5.5 Hz: 1H); 7.25 (broad d, J=8.5 Hz: 2H); 7.68 (broad d, J=8.5 Hz:2H); 7.89 (broad d, J=8.5 Hz: 2H); 7.92 (d, J=5.5 Hz: 1H).

EXAMPLE 2335,5-Dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.5 ml of trifluoroacetic acid is added to a solution of 0.035 g of5,5-dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 0.5 ml of dichloromethane, at a temperature in the region of 20° C.Stirring is continued at this temperature for 5 hours. The reactionmixture is purified by preparative LC/MS. The fractions containing theexpected product are concentrated to dryness under reduced pressure. Theresidue thus obtained is taken up in methanol and then placed on a BondElut Varian cartridge of reference 1225-6027 containing 5 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. 0.015 g of5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichproduct are as follows:

-   m.p.: 161° C.

Mass IE

m/z=410 M⁺. base peak

m/z=395 (M-CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺

m/z=148 C₇H₆N₃O⁺

m/z=107 C₆H₇N₂ ⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 4.46(broad s: 2H); 5.86 (broad s: 2H); 6.46 (broad s: 1H); 6.53 (broad d,J=5.5 Hz: 1H); 7.69 (broad d, J=8.5 Hz: 2H); 7.84 (d, J=5.5 Hz: 1H);7.89 (broad d, J=8.5 Hz: 2H).

EXAMPLE 2345,5-Dimethyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A solution of 0.050 g of5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 5 ml of acetic anhydride is stirred under an inert atmosphere ofargon for 24 hours at a temperature in the region of 80° C. The reactionmixture is purified by preparative LC/MS. The fractions containing theexpected product are concentrated to dryness under reduced pressure. Theresidue thus obtained is taken up in methanol and then placed on a BondElut Varian cartridge of reference 1225-6027 containing 5 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. 0.006 g of5,5-dimethyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichproduct are as follows:

Mass IE

m/z=452 M⁺.

m/z=410 (M-C₂H₂O)⁺. base peak

m/z=395 (m/z=410-CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=150 C₈H₁₀N₂O⁺.

m/z=107 C₆H₇N₂ ⁺.

m/z=43 C₂H₃O⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (broad s: 6H);2.11 (s: 3H); 4.65 (broad s: 2H); 7.15 (broad d, J=5.5 Hz: 1H); 7.68(broad d, J=8.5 Hz: 2H); 7.89 (broad d, J=8.5 Hz: 2H); 8.14 (broad s:1H); 8.27 (d, J=5.5 Hz: 1H); 10.49 (unresolved complex: 1H).

EXAMPLE 2355,5-Dimethyl-1-(2-tert-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.05 g of5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis added portionwise to a solution of 0.029 g of di-tert-butyldicarbonate in 0.65 ml of tert-butyl alcohol, under an inert atmosphereof argon at a temperature in the region of 20° C. Stirring is continuedat this temperature for 24 hours. The reaction mixture is concentratedto dryness under reduced pressure. The residue thus obtained is purifiedby flash chromatography using a cartridge 16 mm in diameter packed with5 g of conditioned 20-40 μm silica, and then eluted with a mixture(cyclohexane/ethyl acetate)(8/2) (v/v). The fractions between 260 and400 ml are concentrated under reduced pressure. 0.035 g of5,5-dimethyl-1-(2-tert-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IC

m/z=511 MH⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 1.49 (s:9H); 4.63 (broad s: 2H); 7.08 (broad dd, J=5.5 and 1.5 Hz: 1H); 7.68(broad d, J=9 Hz: 2H); 7.84 (broad s: 1H); 7.87 (broad d, J=9 Hz: 2H);8.19 (d, J=5.5 Hz: 1H); 9.73 (broad s: 1H).

EXAMPLE 2365,5-Dimethyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.010 ml of methanesulfonyl chloride is added to a solution of 0.050 gof5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 0.4 ml of pyridine, under an inert atmosphere of argon at atemperature in the region of 20° C. Stirring is continued at thistemperature for 2 hours. The reaction mixture is poured into 50 ml ofsaturated sodium bicarbonate solution and then extracted with 2×50 ml ofethyl acetate. The organic phase is dried over magnesium sulfate,filtered and then concentrated to dryness under reduced pressure. 0.020g of5,5-dimethyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white powder, the characteristics ofwhich product are as follows:

-   m.p.: 208° C.

Mass IE

m/z=488 M⁺. base peak

m/z=473 (M-CH₃)⁺

m/z=409 (M-SO₂CH₃)⁺

m/z=219 C₈H₄NOSF₃ ⁺

m/z=185 C₇H₉N₂O₂S⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 3.27(unresolved complex: 3H); 4.63 (broad s: 2H); from 6.95 to 7.10(unresolved complex: 2H); 7.68 (broad d, J=8.5 Hz: 2H); 7.89 (broad d,J=8.5 Hz: 2H); 8.17 (unresolved complex: 1H).

EXAMPLE 2375,5-Dimethyl-1-(2-methoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.056 ml of methyl chloroformate is added to a solution of 0.100 g of5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dionein 1.5 ml of pyridine, under an inert atmosphere of argon at atemperature in the region of 20° C. Stirring is continued at thistemperature for 20 hours. A further 0.56 ml of methyl chloroformate isadded. Stirring is continued at this temperature for 20 hours. Thereaction mixture is taken up in 5 ml of ethyl acetate, and then washedsuccessively with 5 ml of water, ml of saturated sodium chloridesolution and then 5 ml of water. The organic phase is dried overmagnesium sulfate, filtered and then concentrated to dryness underreduced pressure. The residue obtained is purified on a Kromasil C18, 5μm column (100×20 mm), eluting with a linear gradient of from 5% to 95%acetonitrile containing 0.07% (v/v) of trifluoroacetic acid (TFA) inwater containing 0.07% (v/v) TFA, at a flow rate of 10 ml/minute. Thefractions containing the expected product are concentrated to drynessunder reduced pressure. The residue obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.0.024 g of5,5-dimethyl-1-(2-methoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a white solid, the characteristics ofwhich product are as follows:

Mass IE

m/z=468 M⁺. base peak

m/z=453 (M-CH₃)⁺

m/z=410 (M-C₂H₂O₂)⁺

m/z=219 C₈H₄NOSF₃ ⁺.

m/z=166 C₈H₁₀N₂O₂ ⁺.

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.44 (s: 6H); 3.70 (s:3H); 4.65 (broad s: 2H); 7.12 (dd, J=5.5 and 2 Hz: 1H); 7.69 (broad d,J=9 Hz: 2H); 7.89 (broad d, J=9 Hz: 2H); 7.90 (broad s: 1H); 8.23 (d,J=5.5 Hz: 1H); 10.18 (broad s: 1H).

EXAMPLE 2385,5-Dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

0.1 g of sodium hydride is added to a solution of 0.417 g of5,5-dimethyl-3-(3-chloro-4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 20 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 0° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.380 g of2-chloro-4-(bromomethyl)pyridine in 20 ml of anhydrous dimethylformamideis added, followed by addition of ice-cold water after reaction for 10minutes. The reaction mixture is taken up in 400 ml of ethyl acetate andthen washed with 400 ml of water. The organic phase is dried overmagnesium sulfate, filtered and then concentrated to dryness underreduced pressure. The residue thus obtained is purified by flashchromatography using a cartridge 27 mm in diameter packed with 25 g ofconditioned 20-40 μm silica, and then eluted with a mixture(cyclohexane/ethyl acetate)(8/2)(v/v). The fractions between 150 and 350ml are concentrated to dryness under reduced pressure. 0.3 g of5,5-dimethyl-1-(2-chloropyrid-4-yl-methyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IE

m/z=463 M⁺. base peak

m/z=448 (M-CH₃)⁺

m/z=253 C₈H₃NOSClF₃ ⁺.

m/z=167 C₇H₄N₂OCl⁺

m/z=126 C₆H₅Cl⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 4.68(broad s: 2H); 7.49 (broad d, J=5.5 Hz: 1H); 7.63 (broad s: 1H); 7.71(dd, J=9 and 3 Hz: 1H); 7.97 (d, J=3 Hz: 1H); 8.05 (d, J=9 Hz: 1H); 8.38(d, J=5.5 Hz: 1H).

Preparation of5,5-dimethyl-3-(3-chloro-4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dione

A solution of 2 g of 3-chloro-4-trifluoromethylsulfanylaniline in 22 mlof toluene is added over 30 minutes to a suspension of 1.97 g ofdiphosgene and 0.03 g of vegetable charcoal in 22 ml of toluene, at atemperature in the region of −20° C. The mixture is stirred to atemperature in the region of 20° C. and is then refluxed for 3 hours.The mixture is cooled to a temperature in the region of 20° C. and thenfiltered through Celite. 1.35 g of methyl α-aminoisobutyratehydrochloride, 15 ml of toluene and 2.23 ml of triethylamine are addedto the filtrate. The mixture thus obtained is refluxed for 24 hours andthen cooled to a temperature in the region of 20° C. The reactionmixture is concentrated under reduced pressure. The residue obtained ispurified by flash chromatography on a cartridge 37 mm in diameter packedwith conditioned 20-40 μm silica and then eluted with a mixture(cyclohexane/ethyl acetate)(5/5)(v/v). The fractions between 110 and 250ml are concentrated under reduced pressure, and 2 g of5,5-dimethyl-3-(3-chloro-4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneare thus obtained, the characteristics of which product are as follows:

Mass IE

m/z=338 M⁺. base peak

m/z=253 C₈H₃NOSClF₃ ⁺.

m/z=184 (m/z=253-—CF₃)⁺

m/z=84 C₄H₆NO⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.42 (s: 6H); 7.63(dd, J=8.5 and 2.5 Hz: 1H); 7.90 (d, J=2.5 Hz: 1H); 8.02 (d, J=8.5 Hz:1H); 8.75 (unresolved complex: 1H).

EXAMPLE 2395,5-Dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.3 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.2 ml of N-methyl-2-pyrrolidone and 0.4 ml of para-methoxybenzylamineis placed in a Personal Chemistry Emrys Optimiser microwave oven. Themixture is irradiated with magnetic stirring at 200° C. for about 70minutes. The reaction mixture is purified by flash chromatography usinga cartridge 37 mm in diameter packed with 50 g of 20-40 μm conditionedsilica, and then eluted with a mixture (cyclohexane/ethylacetate)(8/2)(v/v). The fractions between 470 and 640 ml areconcentrated to dryness under reduced pressure. 0.091 g of5,5-dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(3-chloro-4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dioneis thus obtained, the characteristics of which are as follows:

Mass IE

m/z=564 M⁺.

m/z=495 (M-—CF₃)⁺

m/z=136 C₈H₁₀NO⁺

m/z=121 C₈HgO⁺ base peak

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.38 (s: 6H); 3.71 (s:3H); 4.39 (d, J=5.5 Hz: 2H); 4.45 (broad s: 2H); 6.48 (broad s: 1H);6.53 (broad d, J=5.5 Hz: 1H); 6.85 (d, J=8.5 Hz: 2H); 6.89 (t, J=5.5 Hz:1H); 7.24 (d, J=8.5 Hz: 2H); 7.69 (dd, J=8.5 and 2.5 Hz: 1H); 7.92 (d,J=5.5 Hz: 1H); 7.95 (d, J=2.5 Hz: 1H); 8.06 (d, J=8.5 Hz: 1H).

EXAMPLE 2405,5-Dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.4 ml of N-methyl-2-pyrrolidone, 0.044 g of ethylamine hydrochlorideand 0.120 ml of triethylamine is placed in a Personal Chemistry EmrysOptimiser microwave oven. The mixture is irradiated with magneticstirring at 200° C. for about 70 minutes. The reaction mixture ispurified by preparative LC/MS. The fractions containing the expectedproduct are concentrated to dryness under reduced pressure. The residuethus obtained is taken up in methanol and then placed on a Bond ElutVarian cartridge of reference 1225-6027 containing 5 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. 0.029 g of5,5-dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which are as follows:

Mass IE

m/z=472 M⁺.

m/z=457 (M-CH₃)⁺ base peak

m/z=429 (M-C₂H₅N)⁺

m/z=403 (M-—CF₃)⁺

m/z=121 C₇H₉N₂ ⁺.

m/z=44 C₂H₆N⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.14 (t, J=7 Hz: 3H);1.43 (s: 6H); 3.27 (mt: 2H); 4.46 (broad s: 2H); 6.38 (broad t, J=5.5Hz: 1H); 6.45 (broad s: 1H); 6.51 (broad d, J=5.5 Hz: 1H); 7.70 (dd,J=8.5 and 2.5 Hz: 1H); 7.92 (d, J=5.5 Hz: 1H); 7.96 (d, J=2.5 Hz: 1H);8.06 (d, J=8.5 Hz: 1H).

EXAMPLE 2415,5-Dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

A sealed 2.5 ml tube containing 0.1 g of5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione,0.5 ml of N-methyl-2-pyrrolidone, 0.030 g of methylamine hydrochlorideand 0.120 ml of triethylamine is placed in a Personal Chemistry EmrysOptimiser microwave oven. The mixture is irradiated with magneticstirring at 200° C. for about 70 minutes. The reaction mixture ispurified by preparative LC/MS. The fractions containing the expectedproduct are concentrated to dryness under reduced pressure. The residuethus obtained is taken up in methanol and then placed on a Bond ElutVarian cartridge of reference 1225-6027 containing 5 g of SCX phaseconditioned with methanol. The cartridge is washed with methanol andthen eluted with 2M ammoniacal methanol. The ammoniacal fractions areconcentrated to dryness under reduced pressure. The residue thusobtained is purified by flash chromatography using a cartridge 20 mm indiameter packed with 10 g of 20-40 μm conditioned silica, and theneluted with dichloromethane at a flow rate of 8 ml/minute. The fractionsbetween 70 and 100 ml are concentrated to dryness under reducedpressure. 0.015 g of5,5-dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of an amorphous white powder, thecharacteristics of which are as follows:

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 2.77 (d,J=5 Hz: 3H); 4.48 (broad s: 2H); 6.40 (broad q, J=5 Hz: 1H); 6.46 (broads: 1H); 6.54 (broad d, J=5.5 Hz: 1H); 7.70 (dd, J=8.5 and 3 Hz: 1H);7.94 (d, J=5.5 Hz: 1H); 7.97 (d, J=3 Hz: 1H); 8.06 (d, J=8.5 Hz: 1H).

EXAMPLE 2425,5-Dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione

3 ml of trifluoroacetic acid are added to a solution of 0.080 g of5,5-dimethyl-1-[2-(4-methoxybenzylamino)pyrid-4-ylmethyl]-3-(3-chloro-4-trifluoromethanesulfanylphenyl)-imidazolidine-2,4-dionein 1 ml of dichloromethane, at a temperature in the region of 20° C.Stirring is continued at this temperature for about 16 hours. Thereaction mixture is concentrated to dryness under reduced pressure. Theresidue obtained is purified by preparative LC/MS. The fractionscontaining the expected product are concentrated to dryness underreduced pressure. The residue thus obtained is taken up in methanol andthen placed on a Bond Elut Varian cartridge of reference 1225-6027containing 5 g of SCX phase conditioned with methanol. The cartridge iswashed with methanol and then eluted with 2M ammoniacal methanol. Theammoniacal fractions are concentrated to dryness under reduced pressure.0.027 g of5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(3-chloro-4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dioneis thus obtained in the form of a powder, the characteristics of whichare as follows:

Mass IE

m/z=444 M⁺. base peak

m/z=429 (M-CH₃)⁺

m/z=148 C₇H₆N₃O⁺

m/z=107 C₆H₇N₂ ⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.43 (s: 6H); 4.46(broad s: 2H); 5.86 (broad s: 2H); 6.46 (broad s: 1H); 6.54 (broad dd,J=5.5 and 1.5 Hz: 1H); 7.70 (dd, J=8.5 and 2.5 Hz: 1H); 7.86 (d, J=5.5Hz: 1H); 7.97 (d, J=2.5 Hz: 1H); 8.06 (d, J=8.5 Hz: 1H).

EXAMPLE 2435,5-Dimethyl-1-(2,6-dibromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)-imidazolidine-2,4-dione

0.036 g of sodium hydride is added to a solution of 0.230 g of5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dionein 2 ml of anhydrous dimethylformamide, under an inert atmosphere ofargon at a temperature in the region of 20° C. Stirring is continued atthis temperature for 30 minutes. A solution of 0.349 g of2,6-dibromo-4-(bromomethyl)pyridine in 3 ml of anhydrousdimethylformamide is added, followed by addition of ice-cold water afterreaction for 20 minutes. The reaction mixture is taken up in ethylacetate and then washed with water. The organic phase is dried overmagnesium sulfate, filtered and then concentrated to dryness underreduced pressure. The residue thus obtained is purified by flashchromatography using a cartridge 27 mm in diameter packed with 25 g of20-40 μm conditioned silica, and then eluted with dichloromethane. Thefractions between 65 and 135 ml are concentrated under reduced pressure.0.25 g of5,5-dimethyl-1-(2,6-dibromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dioneis thus obtained, the characteristics of which product are as follows:

Mass IC

m/z=569 MNH₄ ⁺ base peak

m/z=552 MH⁺

m/z=474 (M-Br 2H)⁺

m/z=396 (m/z=474-Br +H)⁺

¹H NMR spectrum (300 MHz, (CD₃)₂SO d6, δ in ppm): 1.45 (s: 6H); 4.67(broad s: 2H); 7.72 (broad d, J=8 Hz: 2H); 7.83 (s: 2H); 7.89 (broad d,J=8 Hz: 2H).

The compound5,5-dimethyl-3-(4-trifluoromethylsulfanylphenyl)imidazolidine-2,4-dioneis described in Example 211.

Synthesis of the Reagents

REFERENCE EXAMPLE 208a 2-Chloro-4-(bromomethyl)pyridine

A solution of 0.2 g of 2-chloro-4-(hydroxymethyl)pyridine in 2.5 ml ofdichloromethane is added dropwise to a solution of 0.706 g ofdibromotriphenylphosphorane in 9.5 ml of dichloromethane, under an inertatmosphere of argon at a temperature in the region of 20° C. Stirring iscontinued at this temperature for about 1 hour. The reaction medium istaken up in 50 ml of dichloromethane and then washed with 3×50 ml ofwater. The organic phase is dried over magnesium sulfate, filtered andthen concentrated to dryness under reduced pressure. The residue thusobtained is purified by flash chromatography using a cartridge 20 mm indiameter packed with 10 g of 20-40 μm conditioned silica, and theneluted with a mixture (cyclohexane/ethyl acetate)(8/2)(v/v) at a flowrate of 8 ml/minute. The fractions between 8 and 24 ml are concentratedunder reduced pressure. 0.1 g of 2-chloro-4-(bromomethyl)-pyridine isthus obtained.

REFERENCE EXAMPLE 208b 2-chloro-4-(hydroxymethyl)pyridine

2.04 g of sodium borohydride are added portionwise to a solution of 1.7g of ethyl 2-chloropyridine-4-carboxylate in 20 ml of ethanol, under aninert atmosphere of argon at a temperature in the region of 0° C. Thereaction mixture is refluxed with stirring for 3 hours and thenconcentrated to dryness under reduced pressure. The residue thusobtained is taken up in dichloromethane and then washed with water. Theorganic phase is dried over magnesium sulfate, filtered and thenconcentrated to dryness under reduced pressure. 1 g of2-chloro-4-(hydroxymethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 208c Ethyl 2-chloropyridine-4-carboxylate

1 ml of concentrated sulfuric acid is added to a solution of 2.2 g of2-chloropyridine-4-carboxylic acid in 30 ml of ethanol. The reactionmixture is refluxed with stirring for 16 hours and then concentrated todryness under reduced pressure. The residue thus obtained is taken up in30 ml of water and then extracted with 3×30 ml of dichloromethane. Theorganic phase is dried over magnesium sulfate, filtered and thenconcentrated to dryness under reduced pressure. The oil thus obtained ispurified by filtration through 13 g of silica, eluting withdichloromethane. The fractions containing the expected product areconcentrated to dryness under reduced pressure. 2.1 g of ethyl2-chloropyridine-4-carboxylate are thus obtained.

REFERENCE EXAMPLE 209a 2-ethoxy-4-(bromomethyl)pyridine

A solution of 0.31 g of 2-ethoxy-4-(hydroxymethyl)pyridine in 6 ml ofdichloromethane is added dropwise to a solution of 1.025 g ofdibromotriphenylphosphorane in 12 ml of dichloromethane, under an inertatmosphere of argon at a temperature in the region of 20° C. Stirring iscontinued at this temperature for about 1 hour. The reaction medium istaken up in 100 ml of dichloromethane and then washed with 3×100 ml ofwater. The organic phase is dried over magnesium sulfate, filtered andthen concentrated to dryness under reduced pressure. The residue thusobtained is purified by flash chromatography, using a cartridge 27 mm indiameter packed with 20 g of 20-40 μm conditioned silica, and theneluted with a mixture (cyclohexane/ethyl acetate)(9/1)(v/v) at a flowrate of 8 ml/minute. The fractions between 80 and 180 ml areconcentrated under reduced pressure. 0.37 g of2-ethoxy-4-(bromomethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 209b 2-ethoxy-4-(hydroxymethyl)pyridine

0.508 g of sodium borohydride is added portionwise to a solution of0.524 g of ethyl 2-ethoxypyridine-4-carboxylate in 5.2 ml of ethanol,under an inert atmosphere of argon at a temperature in the region of 0°C. The reaction mixture is refluxed with stirring for 3 hours and thenconcentrated to dryness under reduced pressure. The residue thusobtained is taken up in 50 ml of dichloromethane and then washed with 50ml of water. The organic phase is dried over magnesium sulfate, filteredand then concentrated to dryness under reduced pressure. 0.310 g of2-ethoxy-4-(hydroxymethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 209c Ethyl 2-ethoxypyridine-4-carboxylate

0.5 ml of concentrated sulfuric acid is added to a solution of 1 g of2-fluoropyridine-4-carboxylic acid in 15 ml of ethanol. The reactionmixture is refluxed with stirring for 48 hours and then concentrated todryness under reduced pressure. The residue thus obtained is taken up in100 ml of water and then extracted with 3×100 ml of dichloromethane. Theorganic phase is dried over magnesium sulfate, filtered and thenconcentrated to dryness under reduced pressure. The crude product thusobtained is purified by flash chromatography using a cartridge 37 mm indiameter packed with 50 g of 20-40 μm conditioned silica, and theneluted with a mixture (dichloromethane/methanol)(90/10)(v/v), at a flowrate of 8 ml par minute. The fractions between 350 ml and 390 ml areconcentrated under reduced pressure. 0.524 g of ethyl2-ethoxypyridine-4-carboxylate is thus obtained in the form of an oil.

REFERENCE EXAMPLE 210a 2-Ethyl-4-(bromomethyl)pyridine

A solution of 0.3 g of 2-ethyl-4-(hydroxymethyl)pyridine in 3.5 ml ofdichloromethane is added dropwise to a solution of 1.25 g ofdibromotriphenylphosphorane in 4 ml of dichloromethane, under an inertatmosphere of argon at a temperature in the region of 0° C. The mixtureis stirred to a temperature in the region of 20° C. over about 1 hour.The reaction medium is taken up in 50 ml of dichloromethane and thenwashed with 3×50 ml of water. The organic phase is dried over magnesiumsulfate, filtered and then concentrated to dryness under reducedpressure. The residue thus obtained is purified by flash chromatographyusing a cartridge 20 mm in diameter packed with 10 g of 20-40 μmconditioned silica, and then eluted with a mixture (cyclohexane/ethylacetate)(9/1)(v/v), at a flow rate of 8 ml/minute. The fractions between80 and 120 ml are concentrated under reduced pressure. 0.062 g of2-ethyl-4-(bromomethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 210b 2-ethyl-4-(hydroxymethyl)pyridine

5.36 g of sodium borohydride are added portionwise to a solution of 5.08g of ethyl 2-ethylpyridine-4-carboxylate in 53 ml of ethanol, under aninert atmosphere of argon at a temperature in the region of 0° C. Thereaction mixture is refluxed with stirring for 3 hours and thenconcentrated to dryness under reduced pressure. The residue thusobtained is taken up in 500 ml of dichloromethane and then washed with500 ml of water. The organic phase is dried over magnesium sulfate,filtered and then concentrated to dryness under reduced pressure. 3.16 gof 2-ethyl-4-(hydroxymethyl)pyridine are thus obtained.

REFERENCE EXAMPLE 210c Ethyl 2-ethylpyridine-4-carboxylate

2.35 ml of concentrated sulfuric acid are added to a solution of 5 g of2-ethylpyridine-4-carboxylic acid in 75 ml of ethanol. The reactionmixture is refluxed with stirring for about 64 hours and thenconcentrated to dryness under reduced pressure. The residue thusobtained is taken up in 500 ml of water and then extracted with 500 mlof dichloromethane. The organic phase is dried over magnesium sulfate,filtered and then concentrated to dryness under reduced pressure. 5.08 gof ethyl 2-ethylpyridine-4-carboxylate are thus obtained in the form ofan oil.

REFERENCE EXAMPLE 214a 2-bromo-4-(bromomethyl)pyridine

0.073 ml of acetic acid is added to a solution of 0.172 g of2-bromo-4-methylpyridine in 2.5 ml of carbon tetrachloride, under aninert atmosphere of argon at a temperature in the region of 20° C. Themixture brought, with stirring, to a temperature of 50° C. 0.356 g ofN-bromosuccinimide and 0.048 g of benzoyl peroxide are addedsuccessively at this temperature. The mixture is maintained at 80° C.for about 18 hours. After cooling, the reaction medium is placed on acartridge 20 mm in diameter packed with 10 g of 20-40 μm silica notconditioned beforehand, and then eluted with dichloromethane at a flowrate of 5 ml/minute. The fractions between 30 and 40 ml are concentratedto dryness under reduced pressure. 0.071 g of2-bromo-4-(bromomethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 215a 2-Fluoro-4-(bromomethyl)pyridine

0.073 ml of acetic acid is added to a solution of 0.111 g of2-fluoro-4-methylpyridine in 2.5 ml of carbon tetrachloride, under aninert atmosphere of argon at a temperature in the region of 20° C. Themixture is brought, with stirring, to a temperature of 50° C. 0.356 g ofN-bromosuccinimide and 0.048 g of benzoyl peroxide are successivelyadded at this temperature. The mixture is brought to 80° C. over about16 hours. After cooling, the reaction medium is placed on a cartridge 20mm in diameter packed with 10 g of 20-40 μm silica not conditionedbeforehand, and then eluted with dichloromethane at a flow rate of 5ml/minute. The fractions between 28 and 38 ml are concentrated todryness under reduced pressure. 0.063 g of2-fluoro-4-(bromomethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 216a 2-Cyano-4-(bromomethyl)pyridine

0.146 ml of acetic acid is added to a solution of 0.236 g of2-cyano-4-methylpyridine in 5 ml of carbon tetrachloride, under an inertatmosphere of argon at a temperature in the region of 20° C. The mixtureis brought, with stirring, to a temperature of 50° C. 0.712 g ofN-bromosuccinimide and 0.096 g of benzoyl peroxide are successivelyadded at this temperature. The mixture is maintained at 80° C. for about18 hours. After cooling, the reaction medium is placed on a cartridge 27mm in diameter packed with 25 g of 20-40 μm silica not conditionedbeforehand, and then eluted with dichloromethane at a flow rate of 10ml/minute. The fractions between 140 and 175 ml are concentrated todryness under reduced pressure. 0.097 g of2-cyano-4-(bromomethyl)pyridine is thus obtained.

REFERENCE EXAMPLE 243a 2,6-dibromo-4-(bromomethyl)pyridine

A solution of 0.5 g of 2,6-dibromo-4-(hydroxymethyl)pyridine in 7 ml ofdichloromethane is added dropwise to a solution of 0.95 g ofdibromotriphenylphosphorane in 5 ml of dichloromethane, under an inertatmosphere of argon at a temperature in the region of 0° C. The mixtureis stirred to a temperature in the region of 20° C. over about 2 hours.The reaction medium is taken up in 100 ml of dichloromethane and thenwashed with 100 ml of water. The organic phase is dried over magnesiumsulfate, filtered and then concentrated to dryness under reducedpressure. The residue thus obtained is purified by flash chromatographyusing a cartridge 37 mm in diameter packed with 50 g of 20-40 μmconditioned silica, and then eluted with a mixture (cyclohexane/ethylacetate)(9/1)(v/v), at a flow rate of 8 ml/minute.

The fractions between 135 and 200 ml are concentrated under reducedpressure. 0.349 g of 2,6-dibromo-4-(bromomethyl)pyridine is thusobtained.

GENERAL PROCEDURE FOR THE PRODUCTS OF EXAMPLES 244 to 255

A solution of 0.481 mM of anilino derivative in 0.6 ml of toluene isadded to a suspension of 0.064 ml of diphosgene (0.53 mM) and 20 mg ofvegetable charcoal in 1 ml of toluene, at a temperature in the region of−20° C. The mixture is stirred to a temperature in the region of 20° C.,and then refluxed for 3 hours. The mixture is cooled to a temperature inthe region of 20° C. and then filtered through Celite. A solution of 100mg of methyl 2-methyl-2-[(pyrid-4-ylmethyl)amino]propanoate (0.48 mM) in0.6 ml of toluene is added to the filtrate. The mixture thus obtained isrefluxed for 16 hours and then cooled to a temperature in the region of20° C. The precipitate is filtered off and the filtrate is concentratedunder reduced pressure. The residue obtained is purified by preparativeLC/MS.

Summary table of the starting anilino derivatives and of the productsprepared

Empirical Molecular Amount of formula of weight of Name of the anilinoStructure of Name of the the Amount Example the starting derivative theproduct the product product product obtained N^(o) anilino derivativeused (mg) obtained obtained obtained obtained (mg) 2442-NITRO-4-(TRIFLUORO- METHOXY)ANILINE 106.7

5,5-Dimethyl-3-(2-nitro-4- trifluoromethoxyphenyl)-1- pyrid-4-ylmethyl-imidazolidine-2,4-dione 2 C18 H15 F3 N4 O5 424.34 54.2 245 4-(1,1,2,2-TETRAFLUORO- ETHOXY)ANILINE 100.4

5,5-Dimethyl-1-pyrid-4-yl- methyl-3-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]- imidazolidine-2,4-dione 2 C19 H17 F4 N3 O3411.36 32.1 246 4-(DIFLUORO- METHOXY)ANILINE 76.4

3-(4-Difluoromethoxy- phenyl)-5,5-dimethyl-1- pyrid-4-ylmethyl-imidazolidine-2,4-dione 2 C18 H17 F2 N3 O3 361.35 3.9 247 3-CHLORO-4-(TRIFLUORO- METHOXY)ANILINE 101.6

3-(3-Chloro-4-trifluoro- methoxyphenyl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H15 Cl F3 N3 O3 413.79 46.2 2483-BROMO- 4-(TRIFLUORO- METHOXY)ANILINE 122.9

3-(3-Bromo-4-trifluoro- methoxyphenyl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H15 Br F3 N3 O3 458.24 43.2 2492,6-DICHLORO- 4-(TRIFLUORO- METHOXY)ANILINE 118.1

3-(2,6-Dichloro-4-trifluoro- methoxyphenyl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H14 C12 F3 N3 O3 448.23 19.9 2503-CHLORO- 4-(TRIFLUORO- METHYLTHIO)ANILINE 109.3

3-(3-Chloro-4-trifluoro- methylsulfanylphenyl)-5,5-dimethyl-1-pyrid-4-yl- methylimidazolidine-2,4- dione 2 C18 H15 Cl F3 N3O2 S 429.85 33 251 2,2-DIFLUORO-5- AMINOBENZODIOXOLE 83.1

3-(2,2-Difluoro-1,3- benzodioxol-5-yl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H15 F2 N3 O4 375.33 7.4 2522-BROMO- 4-(TRIFLUORO- METHOXY)ANILINE 122.9

3-(2-Bromo-4-trifluoro- methoxyphenyl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H15 Br F3 N3 O3 458.24 21.9 2534-(HEPTA- FLUOROPROPYL- THIO)ANILINE 140.8

3-(4- Heptafluoropropylsulfanyl- phenyl)-5,5-dimethyl-1-pyrid-4-ylmethyl- imidazolidine-2,4-dione 2 C20 H16 F7 N3 O2 S 495.4238.5 254 2-METHYL- 4-(TRIFLUORO- METHOXY)ANILINE 91.8

5,5-Dimethyl-3-(2-methyl- 4-trifluoromethoxyphenyl)- 1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C19 H18 F3 N3 O3 393.37 68.8 2552-CHLORO- 4-(TRIFLUORO- METHOXY)ANILINE 101.6

3-(2-Chloro-4-trifluoro- methoxyphenyl)-5,5- dimethyl-1-pyrid-4-yl-methylimidazolidine-2,4- dione 2 C18 H15 Cl F3 N3 O3 413.79 77.6

Summary table of the physicochemical characteristics of the productsobtained

Description of the mass Description of the Empirical Descriptionspectrum NMR spectrum formula Molecular of the mass (analytical (1H NMRof the weight of spectrum LC/MS) spectrum (300 Example Name of theproduct product the product (electron retention MHz, (CD3)2SO- N°obtained obtained obtained impact) time, m/z d6, ≠in ppm) 2445,5-Dimethyl-3-(2-nitro-4- C18 H15 424.34 m/z = 424 M+. 1.44 (broad s:6H); trifluoromethoxyphenyl)- F3 N4 m/z = 409 4.69 (broad s: 2H);1-pyrid-4-yl- O5 (M − CH3)+ 7.41 (broad d, J = methylimidazolidine-2,4-m/z = 407 5.5 Hz: 2H); 7.98 dione 2 (M − OH)+ (d, J = m/z = 378 8.5 Hz:1H); 8.07 (M − NO2)+. (broad d, J = m/z = 147 8.5 Hz: 1H); 8.29 C9H11N2+(d, J = 2.5 Hz: 1H); m/z = 133 8.56 (broad d, J = C7H5N2O+ 5.5 Hz: 2H)m/z = 92 C6H6N+ base peak 245 5,5-Dimethyl-1-pyrid-4- C19 H17 411.36 m/z= 411 M+. 1.43 (s: 6H); 4.65 ylmethyl-3-[4-(1,1,2,2- F4 N3 base peak (s:2H); 6.85 (tt, J = tetrafluoroethoxy)phenyl]- O3 m/z = 396 51 and 3 Hz:1H); imidazolidine-2,4-dione 2 (M − CH3)+ 7.46 (mt: 4H); m/z = 294 7.62(dt, J = 8.5 and (m/z = 396 − 2.5 Hz: 2H); 8.56 C2H2F4)+ (dd, J = 6 andm/z = 235 1.5 Hz: 2H) C9H5NO2F4+. m/z = 147 C9H11N2+ m/z = 133 C7H5N2O+m/z = 92 C6H6N+ 246 3-(4-Difluoromethoxy- C18 H17 361.35 t = 2.64phenyl)-5,5-dimethyl-1- F2 N3 min pyrid-4-yl- O3 m/z = 362methylimidazolidine-2,4- (M + 1) dione 2 247 3-(3-Chloro-4-trifluoro-C18 H15 413.79 m/z = 413 M+. 1.43 (s: 6H); 4.66 methoxyphenyl)-5,5- C1F3 m/z = 398 (s: 2H); 7.46 (d, J = dimethyl-1-pyrid-4-yl- N3 O3 (M −CH3)+ 6 Hz: 2H); 7.66 methylimidazolidine-2,4- m/z = 237 (dd, J = 8.5and 2.5 dione 2 C8H3NO2C1F3+. Hz: 1H); 7.77 m/z = 147 (broad dd, J = 8.5C9H11N2+ and 1 Hz: 1H); 7.93 m/z = 133 (d, J = C7H5N2O+ 2.5 Hz: 1H);8.55 m/z = 92 (broad d, J = 6 Hz: C6H6N+ 2H) base peak 2483-(3-Bromo-4-trifluoro- C18 H15 458.24 m/z = 457 M+. 1.43 (s: 6H); 4.65methoxyphenyl)-5,5- Br F3 N3 m/z = 442 (s: 2H); 7.46 (broaddimethyl-1-pyrid-4-yl- O3 (M − CH3)+ d, J = 6 Hz: 2H);methylimidazolidine-2,4- m/z = 281 7.68 (dd, J = 8.5 dione 2C8H3NO2BrF3+. and 2.5 Hz: 1H); m/z = 147 7.74 (broad d, J = C9H11N2+ 8.5Hz: 1H); 8.05 m/z = 133 (d, J = C7H5N2O+ 2.5 Hz: 1H); 8.55 m/z = 92 (dd,J = 6 and C6H6N+ 1.5 Hz: 2H) base peak 249 3-(2,6-Dichloro-4- C18 H14448.23 m/z = 447 M+. 1.47 (s: 6H); 4.73 trifluoromethoxyphenyl)- C12 F3m/z = 432 (s: 2H); 7.47 (broad 5,5-dimethyl-1-pyrid-4-yl- N3 O3 (M −CH3)+ d, J = 6 Hz: 2H); methylimidazolidine-2,4- m/z = 412 8.00 (broads: 2H); dione 2 (M − Cl)+ 8.58 (dd, J = 6 and m/z = 271 1.5 Hz: 2H)C8H2NO2C12F3+. m/z = 147 C9H11N2+ m/z = 133 C7H5N2O+ m/z = 92 C6H6N+base peak 250 3-(3-Chloro-4-trifluoro- C18 H15 429.85 m/z = 429 M+. 1.43(s: 6H); 4.66 methylsulfanylphenyl)-5,5- Cl F3 base peak (s: 2H); 7.46(broad dimethyl-1-pyrid-4-yl- N3 O2 S m/z = 414 d, J = 6 Hz: 2H);methylimidazolidine-2,4- (M − CH3)+ 7.70 (dd, J = 8.5 dione 2 m/z = 253and 2 Hz: 1H); 7.97 C8H3NOSC1F3+. (d, J = 2Hz: 1H); m/z = 147 8.05 (d, J= C9H11N2+ 8.5 Hz: 1H); 8.54 m/z = 133 (dd, J = 6 and C7H5N2O+ 1.5 Hz:2H) m/z = 92 C6H6N+ 251 3-(2,2-Difluoro-1,3- C18 H15 375.33 t = 2.80benzodioxol-5-yl)-5,5- F2 N3 min dimethyl-1-pyrid-4-yl- O4 m/z = 376methylimidazolidine-2,4- (M + 1) dione 2 252 3-(2-Bromo-4-trifluoro- C18H15 458.24 m/z = 457 M+. 1.43 (s: 3H); 1.48 (s:methoxyphenyl)-5,5-dimethyl- Br F3 m/z = 414 3H); 4.68 (limit AB,1-pyrid-4-ylmethylimidazolid- N3 O3 (M − CH3)+ J = 17 Hz: 2H); 7.42ine-2,4-dione 2 m/z = 378 (broad d, J = 6 Hz: (M − Br)+ 2H); 7.66 (broaddd, J = base peak 8.5 and 2 Hz: 1H); 7.83 m/z = 350 (d, J = 8.5 Hz: 1H);8.07 (m/z = 378 − (broad d, J = 2 Hz: CO)+ 1H); 8.56 (dd, J = 6 m/z =281 and 1.5 Hz: 2H) C8H3NO2BrF3+. m/z = 244 (m/z = 378 − C7H6N2O)+ m/z =147 C9HHN2+ m/z = 133 C7H5N2O+ m/z = 92 C6H6N+ 253 3-(4- C20 H16 495.42m/z = 495 M+. 1.43 (s: 6H); 4.66 Heptafluoropropylsulfanyl- F7 N3 basepeak (s: 2H); 7.46 (broad phenyl)-5,5-dimethyl-1- O2 S m/z = 480 d, J =6 Hz: 2H); pyrid-4-yl- (M − CH3)+ 7.71 (broad d, J =methylimidazolidine-2,4- m/z = 319 8.5 Hz: 2H); 7.89 dione 2C10H4NOSF7+. (broad d, J = 8.5 m/z = 150 Hz: 2H); 8.55 (dd, (m/z = 319 −J = 6 and 1.5 Hz: C3F7)+ 2H) m/z = 147 C9H11N2+ m/z = 133 C7H5N2O+ m/z =92 C6H6N+ 254 5,5-Dimethyl-3-(2- C19 H18 393.37 m/z = 393 M+. 1.43 and1.44 (2s: methyl-4-trifluoro- F3 N3 base peak 6H in total); 2.21methoxyphenyl)-1-pyrid-4- O3 m/z = 378 (s: 3H); 4.65 (broadylmethylimidazolidine-2,4- (M − CH3)+ s: 2H); 7.36 (broad dione 2 m/z =217 d, J = 8.5 Hz: 1H); C9H6NO2F3+. 7.42 (broad d, J = 6 m/z = 147 Hz:2H); 7.45 C9H11N2+ (broads: 1H); 7.55 m/z = 133 (d, J = 8.5 Hz: 1H);C7H5N2O+ 8.55 (dd, J = 6 and m/z = 92 1.5 Hz: 2H) C6H6N+ 2553-(2-Chloro-4-trifluoro- C18 H15 413.79 m/z = 413 M+. 1.43 (s: 3H); 1.48methoxyphenyl)-5,5- Cl F3 m/z = 398 (s: 3H); 4.67 (broaddimethyl-1-pyrid-4-yl- N3 O3 (M − CH3)+ s: 2H); 7.42 (broadmethylimidazolidine-2,4- m/z = 378 d, J = 6 Hz: 2H); dione 2 (M − Cl)+7.62 (ddd, J = 8.5- base peak 2.5 and 1 Hz: 1H); m/z = 350 7.85 (d, J =(m/z = 378 − 8.5 Hz: 1H); 7.88 CO)+ (broad d, J = m/z = 237 2.5 Hz: 1H);8.57 C8H3NO2C1F3+. (dd, J = 6 and m/z = 147 1.5 Hz: 2H) C9H11N2+ m/z =133 C7H5N2O+ m/z = 92 C6H6N+The products of Examples 256 to 263 were obtained according to theprocedure described above.

EXAMPLE 256 Methyl5-(5-hydroxy-4,4-dimethyl-2-oxo-3-quinolin-4-ylmethylimidazolidin-1-yl)-2-trifluoromethoxybenzoate

1H NMR (DMSO)

(P-31800-112-1): 1.47 ppm (s, 6H); 3.89 ppm (s, 3H); 5.15 ppm (s, 2H);from 7.65 to 7.73 ppm (m, 3H); 7.82 ppm (bt, J=8.5 Hz, 1H); 7.92 ppm(dd, J=2.5-8.5 Hz, 1H); 8.07 ppm (bd, J=8.5 Hz, 1H); 8.17 ppm (d, J=2.5Hz, 1H); 8.26 ppm (bd, J=8.5 Hz, 1H); 8.86 ppm (d, J=4.5 Hz, 1H)

LC/MS: MH⁺=488

EXAMPLE 2573-(3-Bromo-4-trifluoromethoxyphenyl)-5,5-dimethyl-1-quinolin-4-ylmethylimidazolidine-2,4-dione

1H NMR (DMSO)

(P-31800-101-1): 1.45 ppm (s, 6H); 5.15 ppm (s, 2H); from 7.62 to 7.72ppm (m, 4H); 7.80 ppm (bt, J=8.5 Hz, 1H); 8.08 ppm (m, 2H); 8.26 ppm(bd, J=8.5 Hz, 1H); 8.86 ppm (d, J=4.5 Hz).

LC/SM: MH+=508

EXAMPLE 2583-(3-Chloro-4-trifluoromethoxyphenyl)-5,5-dimethyl-1-quinolin-4-ylmethylimidazoline-2,4-dione

1H NMR (DMSO):

P-31800-105-1 NMR No. 6354R: 1.44 ppm (s, 6H); 5.14 ppm (s, 2H); from7.61 to 7.84 ppm (m, 5H); 7.94 ppm (d, J=2.5 Hz, 1H); 8.07 ppm (bd,J=8.5 Hz, 1H); 8.24 ppm (bd, J=8.5

Hz, 1H); 8.83 ppm (d, J=4.5 Hz, 1H).

LC/MS: MH+=464

EXAMPLE 2595-(4,4-Dimethyl-2,5-dioxo-3-quinolin-4-ylmethylimidazolidin-1-yl)-2-trifluoromethyl-benzoicacid

1H NMR (DMSO)

(P-29798-111-1): 1.47 ppm (s, 6H); 5.15 ppm (s, 2H); from 7.62 to 7.72ppm (m, 3H); 7.81 ppm (bt, J=8.5 Hz, 1H); 7.88 ppm (dd, J=2.5-8.5, 1H);8.08 ppm (bt, J=8.5 Hz, 1H); 8.15 ppm (d, J=2.5 Hz, 1H); 8.26 ppm (bd,J=8.5 Hz, 1H); 8.87 ppm (d, J=4.5 Hz, 1H); 13.5 ppm (bs, 1H).

LC/MS: MH⁺=474

EXAMPLE 2605,5-Dimethyl-3-{3-[4-(4-methylpiperazin-1-yl)butyryl]-4-trifluoromethoxyphenyl}-1-quinolin-4-ylmethylimidazolidine-2,4-dione

1H NMR (DMSO)

(P-29798-112-1): 1.51 ppm (s, 6H); 1.97 ppm (m, 2H); 2.82 ppm (s, 3H);from 3.0 to 4.0 ppm (broad multiplet, 12H); 5.35 ppm (s, 2H); 7.63 ppm(dq, J=1.5-8.5 Hz, 1H); 7.75 ppm (dd, J=2.5-8.5 Hz, 1H); 7.82 ppm (d,J=2.5 Hz, 1H); 7.94 ppm (bt, J=8.5 Hz, 1H); 8.10 ppm (m, 2H); 8.39 ppm(bd, J=8.5 Hz, 1H); 8.51 ppm (bd, J=8.5 Hz, 1H); 8.72 ppm (bt, J=5.5 Hz,1H); 9.15 ppm (d, J=5 Hz, 1H); 11.97 ppm (bs, 1H).

MS/EI: M+=612+

EXAMPLE 2615-(5-Hydroxy-4,4-dimethyl-2-oxo-3-quinolin-4-ylmethylimidazolidin-1-yl)-2-trifluoromethoxybenzoicacid

The following are introduced into a 30 ml round-bottomed flask equippedwith a magnetic stirrer and a septum on which is mounted a nitrogeninlet:

-   -   200 mg (0.41 mmol) of ester in 2 ml of ether;    -   8 mg (0.205 mmol) of LiAlH₄, i.e., 8 ml of a 1 M solution in 2        ml of THF.

The reaction medium is stirred at room temperature for 24 hours.

By TLC; 8/2 CH₂Cl₂/EtOAc: a product more polar than the startingmaterial is formed, but starting material remains.

A further 0.5 equivalent of LiAlH₄ is added and the mixture is stirredfor 5 hours. A small amount of starting material still remains, but thereaction mixture is worked up.

The reaction medium is hydrolyzed by adding water thereto, and isextracted with 3 times 10 ml of ethyl acetate. The organic fractions arecombined and dried over magnesium sulfate, and the EtOAc is evaporatedoff.

The crude reaction product is purified using a CH₂Cl₂/EtOAc eluentmixture (9/1). 60 mg of alcohol are thus obtained.

1H NMR (DMSO): 1.19 ppm (s, 3H); 1.24 ppm (s, 3H); 3.86 ppm (s, 3H);4.92 ppm (AB system, J=18 Hz, 2H); 5.36 ppm (s, 1H); 7.51 ppm (dm, J=9.0Hz, 1H); 7.58 ppm (d, J=4.5 Hz, 1H); 7.66 (m, 1H); 7.80 ppm (m, 1H);8.00 ppm (dd, J=2.5-9.0 Hz, 1H); 8.06 ppm (dd, J=1.5-8.5 Hz, 1H); 8.28ppm (dd, J=1.5-8.5 Hz, 1H); 8.33 ppm (d, J=2.5 Hz, 1H); 8.84 ppm (df,J=4.5 Hz, 1H).

LC/MS: MH+=489

EXAMPLE 2624,4-dimethyl-3-quinolin-4-ylmethyl-5-thioxo-1-(4-trifluoromethoxyphenyl)imidazolidin-2-one

The following reaction mixture:

-   317 mg (0.739×10⁻³ mol) of hydantoin SB 31051-139-   78 mg (0.19×10⁻³ mol) of Lawesson's reagent-   1 cm³ of toluene    is refluxed for 9 hours and then cooled, filtered and concentrated    under reduced pressure. A yellow foam is recovered, and is purified    by chromatography several times on silica, with chloroform/acetone    eluent (97/3). 231 mg of pure yellow resin are obtained: Rf=0.38    Th=329 mg Yield=70%

¹H NMR (DMSO) ppm

(P-31051-146-2): 1.57 ppm (s, 6H); 5.24 ppm (s, 2H); 7.57 ppm (m, 2H);7.63 ppm (d, J=4.5 Hz, 1H); 7.70 ppm (m, 3H); 7.81 ppm (bt, J=8.5 Hz,1H); 8.08 ppm (dd, J=1.5-8.5 Hz, 1H); 8.26 ppm (dd, J=1.5-8.5 Hz, 1H);8.86 ppm (d, J=4.5 Hz, 1H).

LC/SM: MH₊=446

EXAMPLE 2635,5-dimethyl-1-quinolin-4-ylmethyl-2-thioxo-3-(4-trifluoromethoxyphenyl)imidazolidin-4-one

The following reaction mixture:

-   0.6 g (mmol) of quinoline derivative-   0.918 g (mmol) of thioisocyanate-   12 cm³ of anhydrous THF-   0.2 cm³ of TEA    is stirred at room temperature for 20 hours.

The mixture is concentrated under reduced pressure and then purified ona 25 g AIT column, eluent 95/5 DCM/acetone.

The product of Rf=0.12 is recovered, i.e., 266 mg

Yield=26%

1H NMR (DMSO)

(P-31051-160-2): 1.55 ppm (s, 6H); 5.56 ppm (s, 2H); 7.55 ppm (m, 3H);7.69 ppm (m, 3H); 7.82 ppm (bt, J=8.5 Hz, 1H); 8.08 ppm (dd, J=1.5-8.5,1H); 8.28 ppm (dd, J=1.5-8.5, 1H); 8.83 ppm (d, J=4.5 Hz, 1H).

MS: M⁼⁴⁴⁵ ⁺

The products of Examples 264 to 332 are described in Table 1 below:these products are prepared as indicated in the experimental section ofthe present patent application and especially as indicated for theproducts of Examples 70 to 200, and thus constitute Examples 264 to 332of the present invention.

EXAMPLE 333 Pharmaceutical Composition

Tablets were prepared corresponding to the following formula:

-   Product of Example 9 . . . 0.2 g-   Excipient for a finished tablet weighing . . . 1 g

(details of the excipient: lactose, talc, starch, magnesium stearate).

EXAMPLE 334 Pharmaceutical Composition

Tablets were prepared corresponding to the following formula:

-   Product of Example 52 . . . 0.2 g-   Excipient for a finished tablet weighing . . . 1 g

(details of the excipient: lactose, talc, starch, magnesium stearate).

Pharmaceutical Composition Examples 333 and 334 above illustrate thepresent invention, it being understood that the same preparations can bemade with other preferred products of the present invention, and formpart of the present invention.

The present invention also comprises as examples the compound of formulaI below: the list below gives the names of compound of formula I asdefined above for which B2 is a pyridyl radical or a quinolyl radical:these products form part of the present invention and may be synthesizedaccording to the processes described above for obtaining the compound offormula I, and especially according to the operating conditionsdescribed for the preparation of Examples 61 to 63:

-   5,5-dimethyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxybenzoylamino)pyrid-4-yl-methyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   4-(2-methylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2,2′-bipyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloropyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoropyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-bromopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-diethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-N-cyclohexyl-N-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-benzoylhydrazino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxybenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-acetamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylacetamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)acetamidopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexanylcarboxamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-methyl-4-piperidinyl)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-furanylcarbonyl)aminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-butoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-diethylaminoethoxycarbonylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chloroanilino)carbonylaminopyridin]-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-pyridylamino)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ureidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-thienyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(dimethylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylphenylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-morpholinylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-pyrrolidinyl)ethoxypyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzyloxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoyloxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-amidinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3,2′-bipyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloropyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoropyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-bromopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-diethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-N-cyclohexyl-N-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-benzoylhydrazino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxybenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-acetamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylacetamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)acetamidopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexanylcarboxamidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-methyl-4-piperidinyl)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-furanylcarbonyl)aminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-butoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-diethylaminoethoxycarbonylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chloroanilino)carbonylaminopyridin]-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-pyridylamino)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ureidopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-thienyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(dimethylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylphenylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-morpholinylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-pyrrolidinyl)ethoxypyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzyloxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoyloxypyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-amidinopyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(1′-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminomethylpyridin)-4-ylmethyl]-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   4-(2-methylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethane    sulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2,2′-bipyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloropyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoropyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-bromopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-diethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-N-cyclohexyl-N-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-benzoylhydrazino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxybenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-acetamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylacetamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)acetamidopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexanylcarboxamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-methyl-4-piperidinyl)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-furanylcarbonyl)aminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-butoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-diethylaminoethoxycarbonylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chloroanilino)carbonylaminopyridin]-4-ylmethyl)-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-pyridylamino)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ureidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaninosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-thienyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(dimethylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylphenylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-morpholinylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-pyrrolidinyl)ethoxypyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzyloxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoyloxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-amidinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3,2′-bipyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloropyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoropyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-bromopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-diethylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-N-cyclohexyl-N-methylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-benzoylhydrazino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorobenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxybenzoylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-acetamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylacetamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)acetamidopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexanylcarboxamidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-methyl-4-piperidinyl)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-furanylcarbonyl)aminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-butoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-diethylaminoethoxycarbonylamino)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chloroanilino)carbonylaminopyridin]-4-ylmethyl)-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminocarbonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-pyridylamino)carbonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ureidopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinosulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-thienyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)sulfonylaminopyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylsulfonylaminopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(dimethylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylphenylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)methylaminocarbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-morpholinylamino)carbonylpyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-pyrrolidinyl)ethoxypyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzyloxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoyloxypyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-amidinopyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminomethylpyridin)-4-ylmethyl]-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   4-(2-methylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2,2′-bipyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloropyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoropyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-bromopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-diethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-acetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylacetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-isopropoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-butoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinocarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminocarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ureidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-anilinosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylpheyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(dimethylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(methylphenylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-methoxyphenyl)methylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-chlorophenyl)methylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4-morpholinylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-phenoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-ethoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzyloxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-benzoyloxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[2-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-amidinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isobutylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorophenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3,2′-bipyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxymethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloropyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoropyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-bromopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-diethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-pyrazol-1-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-acetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylacetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-isopropoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-butoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinocarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminocarbonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ureidopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-anilinosulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzylsulfonylaminopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-hydroxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-tert-butoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxycarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(dimethylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-morpholinocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-phenylpiperazinocarbonyl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(methylphenylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-methoxyphenyl)methylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-chlorophenyl)methylaminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4-morpholinylamino)carbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminocarbonylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-phenoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-ethoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzyloxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-benzoyloxypyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-imidazol-2-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-[3-(1H-tetrazol-5-yl)pyridin]-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-amidinopyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminomethylpyridin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[2-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-isobutylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorophenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3,2′-bipyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxymethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-chloropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-fluoropyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-bromopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-aminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-diethylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-N-cyclohexyl-N-methylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)diethylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-pyrazol-1-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-benzoylhydrazino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzoylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(3-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-chlorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-fluorobenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxybenzoylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-acetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylacetamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazino)acetamidopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-cyclohexanylcarboxamidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(1-methyl-4-piperidinyl)carbonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-furanylcarbonyl)aminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-isopropoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-butoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-diethylaminoethoxycarbonylamino)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chloroanilino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-anilinocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminocarbonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-pyridylamino)carbonylaminopyrid-4-ylmethyl)]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ureidopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-aminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-anilinosulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(2-thienyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)sulfonylaminopyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzylsulfonylaminopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-hydroxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-tert-butoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxycarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(methylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(dimethylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-morpholinocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-phenylpiperazinocarbonyl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenylaminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(methylphenylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-methoxyphenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-chlorophenyl)methylaminocarbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4-morpholinylamino)carbonylpyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-aminocarbonylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-phenoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-ethoxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(1-pyrrolidinyl)ethoxypyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-benzoyloxypyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-imidazol-2-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-[3-(1H-tetrazol-5-yl)pyrid-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-amidinopyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminomethylpyridin)-4-ylmethyl]-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-aminomethylpyrid-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   4-(2-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethoxyphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   4-(2-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfanylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5,5-dimethyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   4-(2-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(2-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(3-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(5-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(6-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(7-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methoxyquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-chloroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-fluoroquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-aminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-methylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-dimethylaminoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   4-(8-piperidinoquinolin)-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;-   5-methyl-1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   5-methyl-1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(2-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(3-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(5-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(6-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(7-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-methylquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-methoxyquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-chloroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-fluoroquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-aminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-methylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-dimethylaminoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione;-   1-(8-piperidinoquinolin-4-ylmethyl)-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione.

TABLE 1 (Ex. 264 to 332) Examples Structures 264

265

266

267

268

269

270

271

272

273

274

275

276

277

278

279

280

281

282

283

284

285

286

287

288

289

290

291

292

293

294

295

296

297

298

299

300

301

302

303

304

305

306

307

308

309

310

311

312

313

314

315

316

317

318

319

320

321

322

323

324

325

326

327

328

329

330

331

332

1. A compound of formula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,heterocyclyl, aryl, phenyl optionally substituted with —NR5R6,heteroaryl, —O-alkenyl, —O-alkynyl, —O-cycloalkyl, —S(O)-alkyl,—S(O)-alkenyl, —S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl, —COOR13, —COOR9,—OCOR13, —OCOR8, NR5R6, CONR5R6, —S(O)_(n)—NR5R6, —NR10-CO—R13, —NHCOR8,—NHS(O)_(n)R8, —NH—S(O)_(n)CF₃, —NR10-SO₂—R13, NH—SO₂—NR5R6,—NR10-CO—NR5R6, —NR10-CS—NR5R6 or —NR10-COOR13, all of which areoptionally substituted, all the alkyl, alkenyl, alkynyl and alkoxy aboveare linear or branched and contain not more than 6 carbon atoms, all thecycloalkyl and heterocyclyl above contain not more than 7 carbon atoms,all the aryl and heteroaryl above contain not more than 10 carbon atoms,all the carbocyclyl, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl,heterocyclyl, aryl and heteroaryl above, and also the ring formed by R5and R6 with the nitrogen atom to which they are attached, are optionallysubstituted with one or more substituents, which may be identical ordifferent, selected from the group consisting of halogen, cyano,hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9, —C(═O)—R8,—NR11R12, —C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,—N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8, —S(O)—R8,—N(R10)-S(O)_(n)—NR11R12 and —S(O)—NR11R12, all the aryl and heteroarylabove are optionally substituted with one or more substituents selectedfrom the group consisting of alkyl, alkoxy and alkylenedioxy, all thecyclic radicals above, and also the ring formed by R5 and R6 with thenitrogen atom to which they are attached, are optionally substitutedwith one or more substituents selected from the group consisting of oxoand thioxo, n is 0 to 2, R8 is alkyl, alkenyl, cycloalkyl,cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl,heteroaryl or heteroarylalkyl, R9 is defined as R8 or is hydrogen, R10is hydrogen or alkyl, R11 and R12, which may be identical or different,are hydrogen, C₃-C₆ cycloalkyl, cycloalkylalkyl, C₁-C₄ alkyl, phenyl, orphenylalkyl, optionally substituted with one or more substituents, whichmay be identical or different, selected from the group consisting ofC₁-C₄ alkyl, halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl, andfree, salified, esterified or amidated carboxyl, or R11 and R12 takentogether with the nitrogen atom to which they are attached form a 5- to7-membered cyclic radical containing one or more hetero atoms chosenfrom O, S, N and NR7, and R13, which may be identical to or differentfrom R5 or R6, is defined as R5 or R6, or a racemic, enantiomeric ordiastereoisomeric isomer form of the compound of formula I, or anaddition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 2. The compound according to claim 1 wherein p is0, R and R1, which may be identical or different, are O or NH, R2 and R3taken together with the carbon atom to which they are attached form a 3-to 10-membered carbocyclyl or a 3- to 10-membered heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7, A1 issingle bond, alkyl, allyl or propynyl, Y and Y1, which may be identicalor different, are such that one of Y and Y1 is selected from the groupconsisting of —OCF₃, —S(O)_(n)CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃and —SO₂NR5R6 and the other of Y and Y1 is selected from the groupconsisting of —OCF₃, —S(O)_(n)CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃,—SO₂NR5R6, hydrogen, halogen, hydroxyl, alkoxy, —NR5R6, alkyl, aryl,heteroaryl, —CF₃, —O-allyl, —O-propynyl, —O-cycloalkyl, —S(O)-allyl,—S(O)-propynyl, —S(O)-cycloalkyl, —CONR5R6 and free, salified oresterified carboxyl, wherein R5 and R6, which may be identical ordifferent, are selected from the group consisting of hydrogen, alkyl,alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl and heteroaryl, orR5 and R6 taken together with the nitrogen atom to which they areattached form a 3- to 10-membered heterocyclyl containing one or morehetero atoms chosen from O, S, N and NR7, A2, which may be identical toor different from A1, is defined as A1 or CO or SO₂, B2 is a saturatedor unsaturated heterocyclyl containing 1 or more identical or differenthetero atoms chosen from O, S, N and NR7, optionally substituted withone or more identical or different substituents defined as Y2, R7 ishydrogen, alkyl, cycloalkyl, phenyl, acyl, —S(O)₂Alk, —S(O)₂Aryl,S(O)₂heteroaryl or —S(O)₂NR5R6 radical, Y2 is hydrogen, halogen,hydroxyl, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl,—O-allyl, —O-propynyl, —O-cycloalkyl, —S(O)_(n)-alkyl, —S(O)_(n)-allyl,—S(O)_(n)-propynyl, —S(O)_(n)-cycloalkyl, —COOR9, —OCOR8, —NR5R6,—CONR5R6, —S(O)_(n)—R5R6, —NHCOR8, —NH—S(O)_(n)R8, —NH—S(O)_(n)CF₃ or—NH—SO₂—NR5R6, all these radicals being optionally substituted, all thecarbocyclyl, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl,aryl and heteroaryl above are optionally substituted with one or moresubstituents, which may be identical or different, selected from thegroup consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro, aryl,heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12, —C(═O)—NR11R12,—N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9, N(R10)-C(═O)—NR11R12,—N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8, —N(R10)-S(O)_(n)—NR11R12 and—S(O)_(n)—NR11R12, and all the aryl and heteroaryl above are optionallysubstituted with one or more substituents selected from the groupconsisting of alkyl and alkylenedioxy radicals, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 3. The compound according to claim 1 wherein pis 0, R and R1, which may be identical or different, are O or NH, R2 andR3 taken together with the carbon atom to which they are attached form a3- to 10-membered carbocyclyl or a 3- to 10-membered heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7, A1 issingle bond, alkyl, allyl or propynyl, Y and Y1, which may be identicalor different, are such that one of Y and Y1 is selected from the groupconsisting of —OCF₃, —S(O)CF₃, S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃ and—SO₂NR5R6 and the other from Y and Y1 is selected from the groupconsisting of —OCF₃, —S(O)_(n)CF₃, S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃,—SO₂NR5R6, hydrogen, halogen, hydroxyl, alkoxy, NR5R6, alkyl, phenyl,optionally substituted pyrazolyl and optionally substituted pyridyl, R5and R6, which may be identical or different, are hydrogen, alkyl,alkenyl, cycloalkyl, heterocyclyl, phenyl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl that contains one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered heterocyclyl containing one or more heteroatoms, which may be identical or different, chosen from O, S, N and NR7,optionally substituted with one or more substituents, which may beidentical or different substituents defined as Y2, R7 is hydrogen or analkyl, cycloalkyl or phenyl radical, Y2 is hydrogen, halogen, hydroxyl,alkyl, alkoxy, cycloalkyl, heterocyclyl, phenyl, heteroaryl,—O-cycloalkyl, —S(O)_(n)-alk, —S(O)_(n)-cycloalkyl, —COOR9, —OCOR8,—NR5R6, —CONR5R6, S(O)_(n)—R5R6, —NHCOR8 or —NH—S(O)_(n)R8, all theseradicals being optionally substituted, all the alkyl, alkenyl, alkynyland alkoxy radicals above being linear or branched and contain not morethan 6 carbon atoms, all the cycloalkyl and heterocyclyl radicals abovecontaining not more than 7 carbon atoms, all the aryl and heteroarylradicals above containing not more than 10 carbon atoms, all thecarbocyclyl, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl,aryl and heteroaryl radicals above being optionally substituted with oneor more radicals, which may be identical or different, chosen fromhalogen atoms and cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl,heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12, —C(═O)—NR11R12,—N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9, N(R10)-C(═O)—NR11R12,—N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8, —N(R10)-S(O)_(n)—NR11R12 and—S(O)_(n)—NR11R12, all the aryl and heteroaryl radicals above areoptionally substituted with one or more radicals chosen from alkyl andalkylenedioxy, n is 0 to 2, R8 is alkyl, cycloalkyl, cycloalkylalkyl,heterocyclyl, heterocyclylalkyl, phenyl or phenylalkyl, R9 is defined asR8 or is hydrogen, R10 is hydrogen or alkyl, and R11 and R12, which maybe identical or different, are hydrogen, C₁-C₄ alkyl or phenyl, whichare optionally substituted with one or more radicals, which may beidentical or different, chosen from halogen, hydroxyl, alkoxy, —CF₃,nitro, phenyl and free, salified, esterified or amidated carboxyl, orR11 and R12 taken together with the nitrogen atom to which they areattached form a 5- to 7-membered cyclic radical containing one or morehetero atoms chosen from O, S, N and NR7, or a racemic, enantiomeric ordiastereoisomeric isomer form of the compound of formula I, or anaddition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 4. The compound according to claim 1 wherein Y andY1, which may be identical or different, are such that one of Y and Y1is selected from the group consisting of OCF₃, —O—CF₂—CHF₂, —O—CHF₂,—O—CH₂—CF₃, —S(O)_(n)CF₃, —S—CF₂—CF₂—CF₃, —S(O)_(n)-alk, —S-Alk-O-Alk,—S-Alk-OH, —S-Alk-CN, —S-Alk-heterocyclyl, —SO₂CHF₂, —SO₂CF₂CF₃,—SO₂NR5R6 and —SF₅, in which Alk is alkyl containing from 1 to 4 carbonatoms, and the other of Y and Y1 is chosen from the group consisting ofhydrogen, halogen, nitro, —NR5R6, free or esterified carboxyl, and—CONR5R6, or the

being optionally substituted with one or more alkyl, which arethemselves optionally substituted, or a racemic, enantiomeric ordiastereoisomeric isomer form of the compound of formula I, or anaddition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 5. The compound according to claim 1 wherein oneof Y and Y1 is hydrogen and the other is chosen from —OCF₃,—S(O)_(n)CF₃, —S(O)_(n)-alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, or aracemic, enantiomeric or diastereoisomeric isomer form of the compoundof formula I, or an addition salt with a mineral or organic acid or witha mineral or organic base thereof.
 6. The compound according to claim 1wherein one of Y and Y1 is hydrogen and the other is chosen from—S(O)_(n)CF₃, —SO-Alk, —S(O)₂Alk, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, ora racemic, enantiomeric or diastereoisomeric isomer form of the compoundof formula I, or an addition salt with a mineral or organic acid or witha mineral or organic base thereof.
 7. The compound according to claim 1wherein one of Y and Y1 is hydrogen and the other is chosen from—S(O)_(n)CF₃, —SO₂CHF₂, —SO₂CF₂CF₃ and —SO₂NR5R6, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 8. The compound according to claim 1 whereinone of Y and Y1 is hydrogen and the other is chosen from —S(O)_(n)CF₃,—SO₂CHF₂ and —SO₂CF₂CF₃, or a racemic, enantiomeric or diastereoisomericisomer form of the compound of formula I, or an addition salt with amineral or organic acid or with a mineral or organic base thereof.
 9. Acompound of formula I wherein

p is 0, R and R1, which may be identical or different, are O or NH, R2and R3 taken together with the carbon atom to which they are attachedform a 3- to 10-membered carbocyclyl or a 3- to 10-membered heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7, A1 issingle bond, alkyl, alkenyl or alkynyl, Y and Y1, which may be identicalor different, are such that one of Y and Y1 is —OCF₃, —O—CF₂—CHF₂,—O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl and the other ofY and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, SO₂NR5R6, —SF₅,—S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy, nitro, —CN,—NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl, —O-alkynyl,—O-cycloalkyl, —S(O)-alkenyl, —S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl,—CONR5R6, or free, salified or esterified carboxyl, or the

that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,heterocyclyl, aryl, phenyl optionally substituted with —NR5R6,heteroaryl, —O-alkenyl, —O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkyl,—S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl, —COOR13,—COOR9, —OCOR13, —OCOR8, NR5R6, CONR5R6, —S(O)_(n)—NR5R6, —NR10-CO—R13,—NHCOR8, —NHS(O)_(n)R8, —NH—S(O)_(n)CF₃, —NR10-SO₂—R13, NH—SO₂—NR5R6,—NR10-CO—NR5R6, —NR10-CS—NR5R6 or —NR10-COOR13, all of which areoptionally substituted, all the alkyl, alkenyl, alkynyl and alkoxy aboveare linear or branched and contain not more than 6 carbon atoms, all thecycloalkyl and heterocyclyl above contain not more than 7 carbon atoms,all the aryl and heteroaryl above contain not more than 10 carbon atoms,all the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl orheteroaryl are optionally substituted with one or more radicals, whichmay be identical or different, chosen from halogen, cyano, hydroxyl,alkoxy, —CF₃, nitro, phenyl, carboxyl which is free, salified,esterified with an alkyl radical or amidated with —NR11aR12a,—C(═O)—R9a, —NR11aR12a, —C(═O)—NR11aR12a, —N(R10a)—C(═O)—R9a,—N(R10a)—C(═O)—OR8a, —N(R10a)—C(═O)—NR11aR12a, —N(R10a)—S(O)_(n)—R9a,—S(O)_(n)—R9a, —N(R10a)—S(O)_(n)—NR11aR12a or —S(O)_(n)—NR11aR12a, allthe aryl and heteroaryl above furthermore being optionally substitutedwith an ethylenedioxy, R8 is alkyl, alkenyl, cycloalkyl,cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl,heteroaryl or heteroarylalkyl, R8a is hydrogen, alkyl, alkenyl, phenyl,phenylalkyl, heteroaryl or heteroarylalkyl, R9 is defined as R8 or ishydrogen, R9a is alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,heterocyclylalkyl, phenyl, phenylalkyl, heteroaryl or heteroarylalkyl,R10 is hydrogen or alkyl, R10a is hydrogen or alkyl, R11a and R12a,which may be identical or different, are hydrogen, alkyl, cycloalkyl,cycloalkylalkyl, phenyl, or phenylalkyl, optionally substituted with oneor more substituents, which may be identical or different, chosen fromhalogen, hydroxyl, C₁-C₄ alkyl and C₁-C₄ alkoxy, or R11a and R12a takentogether with the nitrogen atom to which they are attached form a cyclicradical chosen from pyrrolidyl, piperidyl, piperazinyl, morpholinyl,indolinyl, tetrahydroquinolyl, thiazolidinyl and naphthyridyl, R13,which may be identical to or different from R5 or R6, is defined as R5or R6, or a racemic, enantiomeric or diastereoisomeric isomer form ofthe compound of formula I, or an addition salt with a mineral or organicacid or with a mineral or organic base thereof.
 10. The compoundaccording to claim 1 wherein R1 is O.
 11. The compound according toclaim 1 wherein R is O.
 12. The compound of formula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or heterocyclyl, and theheterocyclyl contains one or more hetero atoms chosen from O, S, N andNR7b, all the above R2 and R3 radicals being optionally substituted withone or more radicals chosen from halogen, cyano, hydroxyl, alkyl andalkoxy containing 1 to 4 carbon atoms, —CF₃, nitro, phenyl, carboxylwhich is free, salified, esterified with alkyl or amidated with—NR11bR12b, —C(═O)—R9b, —NR11bR12b and —C(═O)—NR11bR12b, R7b ishydrogen, alkyl or phenyl, R9b is hydrogen, alkyl, cycloalkyl,cycloalkylalkyl or phenyl, R11b and R12b, which may be identical ordifferent, are hydrogen, alkyl, cycloalkyl or phenyl, or R11b and R12btaken together with the nitrogen atom to which they are attached form anoptionally substituted piperazinyl, A1 is single bond, alkyl, alkenyl oralkynyl, Y and Y1, which may be identical or different, are such thatone of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6,—SF₅ or —S(O)_(n)-alkyl and the other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂,—O—CHF₂, —O—CH₂—CF₃, SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen,hydroxyl, alkoxy, nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃,—O-alkenyl, —O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl,—S(O)_(n)-alkynyl, —S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified oresterified carboxyl, or the

that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7 A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,heterocyclyl, aryl, heteroaryl, —O-alkenyl, —O-alkynyl, —O-cycloalkyl,—S(O)_(n)-alkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —COOR13, —OCOR13, NR5R6, CONR5R6, —S(O)_(n)—NR5R6,—NR10-CO—R13, —NR10-SO₂—R13, NH—SO₂—NR5R6, —NR10-CO—NR5R6,—NR10-CS—NR5R6 or —NR10-COOR13, all of which are optionally substituted,all the alkyl, alkenyl, alkynyl and alkoxy above are linear or branchedand contain not more than 6 carbon atoms, all the cycloalkyl andheterocyclyl above contain not more than 7 carbon atoms, all the aryland heteroaryl above contain not more than 10 carbon atoms, all thecarbocyclyl, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl,aryl and heteroaryl above, and also the ring formed by R5 and R6 withthe nitrogen atom to which they are attached, except for the radicals ofR2 and R3, are optionally substituted with one or more substituents,which may be identical or different, selected from the group consistingof halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl,—C(═O)—OR9, —C(═O)—R8, —NR11R12, —C(═O)—NR11R12, —N(R10)-C(═O)—R8,—N(R10)-C(═O)—OR9, —N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8,—S(O)_(n)—R8, —N(R10)-S(O)_(n)—NR11R12 and —S(O)_(n)—NR11R12, all thearyl and heteroaryl above are optionally substituted with one or moresubstituents selected from the group consisting of alkyl, alkoxy andalkylenedioxy, all the cyclic radicals above, and also the ring formedby R5 and R6 with the nitrogen atom to which they are attached, areoptionally substituted with one or more substituents selected from thegroup consisting of oxo and thioxo, n is 0 to 2, R8 is alkyl, alkenyl,cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl,arylalkyl, heteroaryl or heteroarylalkyl, R9 is defined as R8 or ishydrogen, R10 is hydrogen or alkyl, R11 and R12, which may be identicalor different, are hydrogen, C₃-C₆ cycloalkyl, C₁-C₄ alkyl or phenyloptionally substituted with one or more substituents, which may beidentical or different, selected from the group consisting of halogen,cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl, and free, salified,esterified or amidated carboxyl, or R11 and R12 taken together with thenitrogen atom to which they are attached form a 5- to 7-membered cyclicradical containing one or more hetero atoms chosen from O, S, N and NR7,and R13, which may be identical to or different from R5 or R6, isdefined as R5 or R6, or a racemic, enantiomeric or diastereoisomericisomer form of the compound of formula I, or an addition salt with amineral or organic acid or with a mineral or organic base thereof. 13.The compound according to claim 1 wherein R2 and R3 taken together withthe carbon atom to which they are attached form a 3- to 6-memberedcycloalkyl or heterocyclyl containing a nitrogen atom.
 14. The compoundaccording to claim 1 wherein R2 and R3 taken together with the carbonatom to which they are attached form a cycloalkyl radical containingfrom 3 to 6 carbon atoms or azetidinyl, pyrrolidyl or piperidyl.
 15. Thecompound according to claim 1 wherein R2 and R3 taken together with thecarbon atom to which they are attached form a cycloalkyl containing from3 to 6 carbon atoms.
 16. The compound according to claim 1 wherein R2and R3 taken together with the carbon atom to which they are attachedform a cyclopropyl.
 17. The compound according to claim 1 wherein A1 isa single bond and A2 is chosen from a single bond, a linear or branchedalkyl containing not more than 6 carbon atoms and allyl, propynyl, C═Oand SO₂ radicals, the other substituents of said compound are as definedin claim
 1. 18. The compound according to claim 1 wherein A1 is a singlebond and A2 is chosen from a single bond, alkyl, allyl, propynyl, C═Oand SO₂.
 19. The compound according to claim 1 wherein A1 is a singlebond and A2 is chosen from alkyl, allyl, propynyl, C═O and SO₂.
 20. Thecompound according to claim 1 wherein A1 is a single bond and A2 isalkyl or C═O.
 21. The compound according to claim 1 wherein A1 is asingle bond and A2 is C═O, ethylene or methylene.
 22. The compoundaccording to claim 1 wherein A1 is a single bond and A2 is methylene.23. The compound according to claim 1 wherein Y and Y1 are such that oneis hydrogen, halogen or amino and the other is chosen from —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SF₅, —S(O)_(n)—CF₃, —S(O)_(n)-alk,—SO₂CHF₂, —SO₂CF₂CF₃, —SO₂NH₂, —S—CF₂—CF₂—CF₃, —S-Alk-O-Alk, —S-Alk-OH,—S-Alk-CN, —S-Alk-morpholino, —S-Alk-pyrrolidinyl and—S-Alk-piperazinyl, wherein the morpholino, pyrrolidinyl and piperazinylare optionally substituted with Alk, in which Alk is alkyl containingfrom 1 to 4 carbon atoms.
 24. The compound according to claim 1 whereinY is hydrogen and Y1 is chosen from —OCF₃, S(O)_(n)—CF₃, —S(O)_(n)—CH₃,—SO₂CHF₂ and —SO₂NH₂.
 25. The compound according to claim 1 wherein Y ishydrogen and Y1 is chosen from —OCF₃, —S(O)_(n)—CF₃ and —SO₂CHF₂. 26.The compound according to claim 1 wherein Y is hydrogen and Y1 is chosenfrom —OCF₃ and S(O)_(n)—CF₃.
 27. The compound according to claim 1wherein Y is hydrogen and Y1 is chosen from —OCF₃, S—CF₃ and S(O)₂—CF₃.28. The compound according to claim 1 wherein B2 is monocyclic orbicyclic heteroaryl chosen from pyridyl, pyrimidinyl, quinolyl,azaindolyl, 1H-pyrrolo[2,3-b]pyridinyl, quinazolyl, thiazolyl,imidazolyl, pyrazolyl, furazanyl, isoxazolyl, morpholinyl, pyrrolidinyl,furyl, piperidyl, thienyl, chromenyl, oxochromenyl, indolyl, pyrrolyl,purinyl, benzoxazinyl, benzimidazolyl and benzofuranyl, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.
 29. The compound according to claim 1 wherein B2 isheteroaryl chosen from 3- or 4-pyridyl, 3- or 4-quinolyl, imidazolyl,thiazolyl, indolyl, pyrazolyl, pyrrolyl, pyrimidyl, purinyl,benzoxazinyl, benzimidazolyl and benzofuranyl, which are optionallysubstituted with one or more radicals chosen from the definition of Y2.30. The compound according to claim 1 wherein B2 is heteroaryl chosenfrom 4-pyridyl, 4-quinolyl, imidazolyl, thiazolyl, pyrazolyl, pyrrolyl,pyrimidyl and purinyl radicals, which are optionally substituted withone or more radicals chosen from the definition of Y2.
 31. The compoundaccording to claim 1 wherein B2 is heteroaryl chosen from 3- or4-pyridyl, pyrimidinyl, 3- or 4-quinolyl, azaindolyl, quinazolyl,thiazolyl, imidazolyl, pyrazolyl, furazanyl and isoxazolyl, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.
 32. The compound according to claim 1 wherein B2 isheteroaryl chosen from 3- or 4-pyridyl, pyrimidyl, 3- or 4-quinolyl,azaindolyl and quinazolyl, which are optionally substituted with one ormore radicals chosen from the definition of Y2.
 33. The compoundaccording to claim 1 wherein B2 is 4-pyridyl, 4-quinolyl or1H-pyrrolo[2,3-b]pyrid-4-yl, which are optionally substituted with oneor more radicals chosen from the definition of Y2.
 34. The compoundaccording to claim 1 wherein Y2 is 2-amino-4-pyridyl in which the aminois optionally substituted as indicated for the radical —NR5R6 as definedin claim
 1. 35. The compound of formula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

 that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, A2, which may be identical to ordifferent from A1, is defined as A1 or is CO or SO₂, B2 is a saturatedor unsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, phenyl, —COOH,—COOAlk, —CONR5R6, —NR5R6, —NR10-COOR6, —NR10-CO—R6, —NR10-CS—NR5R6,—NR10-CO—NR5R6 or —NR10-SO₂—R6, which are all optionally substituted, R5and R6, which may be identical or different, are chosen from hydrogen,alkyl, cycloalkyl, phenyl and 5- or 6-membered heteroaryl containing 1to 3 hetero atoms chosen from O, N and S, which are all optionallysubstituted, or R5 and R6 taken together with the nitrogen atom to whichthey are attached form an optionally substituted pyrrolidinyl,piperidyl, piperazinyl, morpholinyl or quinazolinyl, R10 is hydrogen oralkyl, all the alkyl, alkoxy, cycloalkyl and phenyl of Y2, R5, R6 andR10, and also the ring formed by R5 and R6 with the atom to which theyare attached, are optionally substituted with one or more radicals,which may be identical or different, chosen from halogen, cyano,hydroxyl, alkyl, alkoxy, OCF₃, —CF₃, —S(O)_(n)—CF₃, nitro, oxo, thioxo,—OCOAlk; and phenyl, which is optionally substituted with one or moreradicals chosen from halogen, alkyl, alkoxy; —OCOAlk; —NH₂, —NHAlk,—N(Alk)₂, —N(alk)(phenylalkyl), —N(Alk)(aminoalkyl),—N(Alk)(alkylaminoalkyl), —N(Alk)(dialkylaminoalkyl), and carboxyl infree form or esterified with an alkyl, all Y2, R5, and R6 phenyl areoptionally substituted with alkylenedioxy, all Y2, R5, R6, and R10 alkylare optionally substituted with one or more saturated or partiallyunsaturated 4- to 7-membered heterocyclyl containing at least onenitrogen atom N and 0 to 2 other hetero atoms chosen from O, N and S,all the pyrrolidinyl and quinazolinyl of Y2, R5, and R6 are optionallysubstituted with oxo or thioxo, all the aryl and heteroaryl abovecontain not more than 10 carbon atoms, except for the radicals of Y2,R5, R6 and R10, all the carbocyclyl, heterocyclyl, alkyl, alkenyl,alkynyl, alkoxy, cycloalkyl, aryl and heteroaryl above, are optionallysubstituted with one or more substituents, which may be identical ordifferent, selected from the group consisting of halogen, cyano,hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9, —C(═O)—R8,—NR11R12, —C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,—N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8, —S(O)_(n)—R8,—N(R10)-S(O)_(n)—NR11R12 and —S(O)_(n)—NR11R12, except for the radicalsof Y2, R5, and R6, all the aryl and heteroaryl above are optionallysubstituted with one or more substituents selected from the groupconsisting of alkyl, alkoxy and alkylenedioxy, except for the radicalsof Y2, R5, and R6, all the cyclic radicals above are optionallysubstituted with one or more substituents selected from the groupconsisting of oxo and thioxo, all the alkyl alkenyl, alkynyl and alkoxybeing linear or branched and containing not more than 6 carbon atoms,all the cycloalkyl and heterocyclyl containing not more than 7 carbonatoms, n is 0 to 2, R8 is alkyl, alkenyl, cycloalkyl, cycloalkylalkyl,heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl orheteroarylalkyl, R9 is defined as R8 or is hydrogen, R11 and R12, whichmay be identical or different, are hydrogen, C₃-C₆ cycloalkyl, C₁-C₄alkyl or phenyl, optionally substituted with one or more substituents,which may be identical or different, selected from the group consistingof halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro, phenyl, and free,salified, esterified or amidated carboxyl, or R11 and R12 taken togetherwith the nitrogen atom to which they are attached form a 5- to7-membered cyclic radical containing one or more hetero atoms chosenfrom O, S, N and NR7, and R13, which may be identical to or differentfrom R5 or R6, is defined as R5 or R6, or a racemic, enantiomeric ordiastereoisomeric isomer form of the compound of formula I, or anaddition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 36. The compound according to claim 1 wherein R5and R6 are pyridyl, pyrazinyl, pyrimidinyl, thienyl, thiazolyl oroxazolyl, which are all optionally substituted.
 37. The compound offormula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

 that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,heterocyclyl, aryl, heteroaryl, —O—alkenyl, —O-alkynyl, —O-cycloalkyl,—S(O)_(n)-alkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —COOR13, —OCOR13, NR5R6, CONR5R6, —S(O)—NR5R6,—NR10-CO—R13, —NR10-SO₂—R13, NH—SO₂—NR5R6, —NR10-CO—NR5R6,—NR10-CS—NR5R6 or —NR10-COOR13, all of which are optionally substituted,all the alkyl, alkenyl, alkynyl and alkoxy above are linear or branchedand contain not more than 6 carbon atoms, all the cycloalkyl andheterocyclyl above contain not more than 7 carbon atoms, all the aryland heteroaryl above contain not more than 10 carbon atoms, all thealkyl above are optionally substituted with heterocyclyl chosen fromthiomorpholin-4-yl, thiazolidin-3-yl, azetidin-1-yl, piperazinyl,imidazolyl, morpholinyl, pyrrolidinyl, piperidyl and azepanyl, all ofwhich are optionally substituted with one or more radicals chosen fromalkyl, hydroxyalkyl, oxo, pyridyl and phenyl optionally substituted withone or more radicals chosen from halogen, alkyl, hydroxyl, alkoxy, —CN,carboxyl or amino, which are themselves optionally substituted, all thecarbocyclyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryland heteroaryl above, and also the ring formed by R5 and R6 with thenitrogen atom to which they are attached, are optionally substitutedwith one or more substituents, which may be identical or different,selected from the group consisting of halogen, cyano, hydroxyl, alkoxy,—CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12,—C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,—N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8, —S(O)—R8,—N(R10)-S(O)—NR11R12 and —S(O)—NR11R12, all the aryl and heteroarylabove are optionally substituted with one or more substituents selectedfrom the group consisting of alkyl, alkoxy and alkylenedioxy, all thecyclic radicals above, and also the ring formed by R5 and R6 with thenitrogen atom to which they are attached, are optionally substitutedwith one or more substituents selected from the group consisting of oxoand thioxo, n is 0 to 2, R8 is alkyl, alkenyl, cycloalkyl,cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl,heteroaryl or heteroarylalkyl, R9 is defined as R8 or is hydrogen, R10is hydrogen or alkyl, R11 and R12, which may be identical or different,are hydrogen, C₃-C₆ cycloalkyl, C₁-C₄ alkyl, or phenyl, optionallysubstituted with one or more substituents, which may be identical ordifferent, selected from the group consisting of halogen, cyano,hydroxyl, alkoxy, —CF₃, nitro, phenyl, and free, salified, esterified oramidated carboxyl, or R11 and R12 taken together with the nitrogen atomto which they are attached form a 5- to 7-membered cyclic radicalcontaining one or more hetero atoms chosen from O, S, N and NR7, andR13, which may be identical to or different from R5 or R6, is defined asR5 or R6, or a racemic, enantiomeric or diastereoisomeric isomer form ofthe compound of formula I, or an addition salt with a mineral or organicacid or with a mineral or organic base thereof.
 38. The compound offormula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

 that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, A2, which may be identical to ordifferent from A1, is defined as A1 or is CO or SO₂, B2 is a saturatedor unsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, phenyl, —CONR5R6,—NR5R6, —NR10-COOH, —NR10-COOAlk, NR10-CO—R6, —NR10-CS—NR5R6,—NR10-CO—NR5R6 or —NR10-SO₂—R6, R5 and R6, which may be identical ordifferent, are chosen from hydrogen; alkyl; cycloalkyl; phenyl;pyrimidinyl; thienyl; pyridyl; quinolyl; thiazolyl optionallysubstituted with one or two halogen; pyran optionally substituted withone or more —OCOAlk; phenyl substituted with one or more radicals chosenfrom halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino andcarboxyl in free form or esterified with an alkyl radical; alkylsubstituted with phenyl, which is itself optionally substituted with oneor more radicals chosen from halogen, alkyl, alkoxy, amino, alkylamino,dialkylamino, carboxyl in free form or esterified with an alkyl radical;alkyl substituted with piperazinyl, which is itself optionallysubstituted with one or more radicals chosen from Alk, Alk-OH andpyridyl; alkyl substituted with imidazolyl; alkyl substituted with oneor more radicals chosen from —NH₂, —NHAlk, —N(Alk)₂,—N(alk)(phenylalkyl), —N(Alk)(aminoalkyl), —N(Alk)(alkylaminoalkyl) and—N(Alk)(dialkylaminoalkyl); alkyl substituted with morpholinyloptionally substituted with one or two Alk; alkyl substituted withpyrrolidinyl; alkyl substituted with piperidyl, which is itselfoptionally substituted with one or two Alk; alkyl substituted withthiomorpholinyl; alkyl substituted with azetidinyl; and alkylsubstituted with azepanyl, which is optionally substituted with oxo, orR5 and R6 taken together with the nitrogen atom to which they areattached form pyrrolidinyl; piperidyl; piperazinyl; morpholinyl; orquinazolinyl, all of which are optionally substituted with one or moreradicals, which may be identical or different, chosen from halogen,alkyl, hydroxyl and alkoxy, and phenyl which is optionally substitutedwith one or more radicals chosen from halogen, alkyl and alkoxy, thepyrrolidinyl and quinazolinyl are optionally substituted with oxo orthioxo, the piperazinyl itself is optionally substituted with one ormore radicals chosen from Alk, Alk-OH and pyridyl, except for theradicals of Y2, R5, R6 and R10, all the carbocyclyl, alkyl, alkenyl,alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl and heteroaryl above,are optionally substituted with one or more substituents, which may beidentical or different, selected from the group consisting of halogen,cyano, hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9,—C(═O)—R8, —NR11R12, —C(═O)—NR11R12, —N(R10)-C(═O)—R8,—N(R10)-C(═O)—OR9, —N(R10)-C(═O)—NR11R12, —N(R10)-S(O)—R8, —S(O)—R8,—N(R10)-S(O)—NR11R12 and —S(O)—NR11R12, except for the radicals of Y2,R5, and R6, all the aryl and heteroaryl above are optionally substitutedwith one or more substituents selected from the group consisting ofalkyl, alkoxy and alkylenedioxy, except for the radicals of Y2, R5, andR6, all the cyclic radicals above, are optionally substituted with oneor more substituents selected from the group consisting of oxo andthioxo, R10 is hydrogen or alkyl, all alkyl, Alk, alkenyl, alkynyl andalkoxy above being linear or branched and containing not more than 6carbon atoms, all the cycloalkyl and heterocyclyl containing not morethan 7 carbon atoms, all the aryl and heteroaryl above contain not morethan 10 carbon atoms, all the phenyl of Y2, R5, and R6 are optionallysubstituted with a radical chosen from —CF₃, —OCF₃, nitro andalkylenedioxy, n is 0 to 2, R8 is alkyl, alkenyl, cycloalkyl,cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl,heteroaryl or heteroarylalkyl, R9 is defined as R8 or is hydrogen, R11and R12, which may be identical or different, are hydrogen, C₃-C₆cycloalkyl, C₁-C₄ alkyl or phenyl, optionally substituted with one ormore substituents, which may be identical or different, selected fromthe group consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro,phenyl, and free, salified, esterified or amidated carboxyl, or R11 andR12 taken together with the nitrogen atom to which they are attachedform a 5- to 7-membered cyclic radical containing one or more heteroatoms chosen from O, S, N and NR7, and R13, which may be identical to ordifferent from R5 or R6, is defined as R5 or R6, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 39. The compound according to claim 1 in which-A2-B2-Y2 is selected from the following radicals:

wherein NR14R15 is defined as —NR5R6 and the definition for Alkyl, Aryland Heteroaryl are chosen from the values of the alkyl, aryl andheteroaryl as defined in claim 1 and optionally substituted as definedin claim
 1. 40. The compound according to claim 1 wherein B2 is selectedfrom the group consisting of 4-pyridyl and 4-quinolyl, which areoptionally substituted with one or more radicals chosen from thedefinition of Y2.
 41. The compound of formula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

 that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 is V1,halogen, hydroxyl, —C(═NH)NH₂, OV1, O—CO-V1, COOV1, COV1, CO—NV1V2,—NV1V2, —NH—CO-V1, —NH—COO-V1, —NH—NH—CO-V1, —NV1-CO—NV1V2,—NV1-CO—NHV1, —NH—CO—NHV1, —NH—SO₂—NHV1 and —NH—SO₂-V1, in which V1 andV2, which may be identical or different, are hydrogen, alkyl, cycloalkylor phenyl or heterocyclyl, all the alkyl, phenyl and heterocyclyl of V1and V2 being optionally substituted with one or more radicals chosenfrom halogen, hydroxyl, alkyl, alkoxy, —CF₃, NH₂, NH-alk, N(Alk)₂ andphenyl, itself optionally substituted with one or more substituentschosen from halogen, hydroxyl and alkoxy radicals, all the phenyl andheterocyclyl of V1 and V2 are optionally substituted with one or morealkyl, the phenyl of V1 and V2 is optionally substituted with —NR5R6,all the alkyl, alkenyl, alkynyl and alkoxy above are linear or branchedand contain not more than 6 carbon atoms, all the cycloalkyl andheterocyclyl above contain not more than 7 carbon atoms, all the aryland heteroaryl above contain not more than 10 carbon atoms, except forV1 and V2, all the carbocyclyl, alkenyl, alkynyl, alkoxy, cycloalkyl,aryl and heteroaryl above, and also the ring formed by R5 and R6 withthe nitrogen atom to which they are attached, are optionally substitutedwith one or more substituents, which may be identical or different,selected from the group consisting of halogen, cyano, hydroxyl, alkoxy,—CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12,—C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,—N(R10)-C(═O)—NR11R12, —N(R10)-S(O)_(n)—R8, —S(O)—R8,—N(R10)-S(O)—NR11R12 and —S(O)—NR11R12, except for V1 and V2, all thearyl and heteroaryl above are optionally substituted with one or moresubstituents selected from the group consisting of alkyl, alkoxy andalkylenedioxy, except for V1 and V2, all the cyclic radicals above, andalso the ring formed by R5 and R6 with the nitrogen atom to which theyare attached, are optionally substituted with one or more substituentsselected from the group consisting of oxo and thioxo, n is 0 to 2, R8 isalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, R9 isdefined as R8 or is hydrogen, R10 is hydrogen or alkyl, R11 and R12,which may be identical or different, are hydrogen, C₃-C₆ cycloalkyl,C₁-C₄ alkyl or phenyl, optionally substituted with one or moresubstituents, which may be identical or different, selected from thegroup consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro,phenyl, and free, salified, esterified or amidated carboxyl, or R11 andR12 taken together with the nitrogen atom to which they are attachedform a 5- to 7-membered cyclic radical containing one or more heteroatoms chosen from O, S, N and NR7, and R13, which may be identical to ordifferent from R5 or R6, is defined as R5 or R6, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 42. The compound of formula I:

wherein p is 0, R and R1, which may be identical or different, are O orNH, R2 and R3 taken together with the carbon atom to which they areattached form a 3- to 10-membered carbocyclyl or a 3- to 10-memberedheterocyclyl containing one or more hetero atoms chosen from O, S, N andNR7, A1 is single bond, alkyl, alkenyl or alkynyl, Y and Y1, which maybe identical or different, are such that one of Y and Y1 is —OCF₃,—O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SO₂NR5R6, —SF₅ or —S(O)_(n)-alkyl andthe other of Y and Y1 is —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃,SO₂NR5R6, —SF₅, —S(O)_(n)-alkyl, hydrogen, halogen, hydroxyl, alkoxy,nitro, —CN, —NR5R6, alkyl, aryl, heteroaryl, —CF₃, —O-alkenyl,—O-alkynyl, —O-cycloalkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —CONR5R6, or free, salified or esterifiedcarboxyl, or the

 that is optionally substituted with one or more alkyl that areoptionally substituted, q is 2, 3 or 4, R5 and R6, which may beidentical or different, are hydrogen, alkyl, alkenyl, alkynyl,cycloalkyl, cycloalkenyl, heterocyclyl, aryl or heteroaryl, or R5 and R6taken together with the nitrogen atom to which they are attached form a3- to 10-membered heterocyclyl containing one or more hetero atomschosen from O, S, N and NR7, A2, which may be identical to or differentfrom A1, is defined as A1 or is CO or SO₂, B2 is a saturated orunsaturated 3- to 10-membered monocyclic or bicyclic heterocyclylcontaining one or more hetero atoms chosen from O, S, N and NR7 that isoptionally substituted with one or more identical or differentsubstituents defined as Y2, R7 is hydrogen, alkyl, cycloalkyl, phenyl,acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or —S(O)₂NR5R6, Y2 ishydrogen, halogen, alkyl, cycloalkyl, hydroxyl, alkoxy, carboxyl whichis free or esterified with an alkyl or phenyl, —NH₂, —NHalk, —N(Alk)₂ orphenyl, all the Y2 alkyl, alkoxy and phenyl are optionally substitutedwith one or more radicals chosen from halogen, hydroxyl, C₁-C₄ alkyl,C₁-C₄ alkoxy, —CF₃, —NH₂, —NH-alk, N(Alk)₂ and phenyl, which is itselfoptionally substituted with one or more substituents chosen fromhalogen, hydroxyl and alkoxy, all the Y2 phenyl are optionallysubstituted with one or more C₁-C₄ alkyl and optionally substituted with—NR5R6, all the alkyl, alkenyl, alkynyl and alkoxy above are linear orbranched and contain not more than 6 carbon atoms, all the cycloalkyland heterocyclyl above contain not more than 7 carbon atoms, all thearyl and heteroaryl above contain not more than 10 carbon atoms, exceptfor Y2, all the carbocyclyl, heterocyclyl, alkyl, alkenyl, alkynyl,alkoxy, cycloalkyl, aryl and heteroaryl above, and also the ring formedby R5 and R6 with the nitrogen atom to which they are attached, areoptionally substituted with one or more substituents, which may beidentical or different, selected from the group consisting of halogen,cyano, hydroxyl, alkoxy, —CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9,—C(═O)—R8, —NR11R12, —C(═O)—NR11R12, —N(R10)-C(═O)—R8,—N(R10)-C(═O)—OR9, —N(R10)-C(═O)—NR11R12, —N(R10)-S(O)—R8, —S(O)—R8,—N(R10)-S(O)—NR11R12 and —S(O)—NR11R12, except for Y2, all the aryl andheteroaryl above are optionally substituted with one or moresubstituents selected from the group consisting of alkyl, alkoxy andalkylenedioxy, except for Y2, all the cyclic radicals above, and alsothe ring formed by R5 and R6 with the nitrogen atom to which they areattached, are optionally substituted with one or more substituentsselected from the group consisting of oxo and thioxo, n is 0 to 2, R8 isalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, R9 isdefined as R8 or is hydrogen, R10 is hydrogen or alkyl, R11 and R12,which may be identical or different, are hydrogen, C₃-C₆ cycloalkyl,C₁—C₄ alkyl or phenyl, optionally substituted with one or moresubstituents, which may be identical or different, selected from thegroup consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro,phenyl, and free, salified, esterified or amidated carboxyl, or R11 andR12 taken together with the nitrogen atom to which they are attachedform a 5- to 7-membered cyclic radical containing one or more heteroatoms chosen from O, S, N and NR7, and R13, which may be identical to ordifferent from R5 or R6, is defined as R5 or R6, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 43. The compound according to claim 1 whereinY2 is hydrogen, F, Cl, —CH₃, —CH₂CH₃, —OH, —OCH₃, —NH₂, —NH-Alk andphenyl optionally substituted with —NR5R6 in which R5 and R6 are asdefined in claim
 1. 44. The compound according to claim 1 wherein B2 isselected from 4-pyridyl and 4-quinolyl substituted with one or tworadicals chosen from F, Cl, —OH and —OCH₃.
 45. The compound according toclaim 1 wherein

is selected from the group consisting of:


46. The compound according to claim 1 wherein -A2-B2-Y2 are selectedfrom the following radicals:


47. The compound of formula (IC):

in which YC and Y1C are such that one is hydrogen, halogen, or amino andthe other is chosen from —OCF₃, —O—CF₂—CHF₂, —O—CHF₂, —O—CH₂—CF₃, —SF₅,—S(O)—CF₃, —S(O)_(n)-alk, —SO₂CHF₂, SO₂CF₂CF₃, —SO₂NH₂, —S—CF₂—CF₂—CF₃,—S-Alk-O-Alk, —S-Alk-OH, —S-Alk-CN, —S-Alk-morpholino, —S-Alk-pyrrolidyland —S-Alk-piperazinyl, the morpholino, pyrrolidyl and piperazinyl areoptionally substituted with Alk, with Alk being alkyl containing from 1to 4 carbon atoms, or the phenyl thereof with its substituents YC andY1C forms one of the two following radicals:

R2C and R3C taken together with the carbon atom to which they areattached form a C₃-C₁₀ cycloalkyl or heterocyclyl, A2C is single bond orCH₂, B2C is pyridyl, pyrimidyl, quinolyl, azaindolyl, quinazolyl,thiazolyl, imidazolyl, pyrazolyl, furazanyl, isoxazolyl, morpholinyl,pyrrolidyl, furyl, piperidyl, chromenyl, oxochromenyl, quinazolyl,thienyl, indolyl, pyrrolyl, purinyl, benzoxazinyl, benzimidazolyl orbenzofuryl, that are optionally substituted with one or more radicalschosen from the definition of Y2C, Y2C is hydrogen, halogen, hydroxyl,cyano, alkyl, alkoxy, phenyl, —COON, —COOAlk, —CONR5R6, —NR5R6,—NR10-COOH, —NR10-COOAlk, NR10-CO—R6, —NR10-CS—NR5R6, —NR10-CO—NR5R6 orNR10-SO₂—R6, all these radicals are optionally substituted, R5 and R6,which may be identical or different, are chosen from hydrogen, alkyl,cycloalkyl, phenyl, pyrimidyl, thienyl, pyridyl, quinolyl, thiazolyl andpyran, all these radicals are optionally substituted, or R5 and R6 takentogether with the nitrogen atom to which they are attached form anoptionally substituted pyrrolidyl, piperidyl, piperazinyl, morpholinylor quinazolinyl, R10 is hydrogen or alkyl, all the alkyl, Alk or ALK,alkoxy, cycloalkyl and phenyl radicals, and also the ring formed by R5and R6 with the atom to which they are attached, are optionallysubstituted with one or more radicals, which may be identical ordifferent, chosen from halogen, cyano, hydroxyl, alkyl, alkoxy, —OCF₃,—CF₃, —S(O)—CF₃, nitro, oxo, thioxo, —OCOAlk, and phenyl, itselfoptionally substituted with one or more radicals chosen from halogen,alkyl, alkoxy; —OCOAlk; —NH₂, —NHAlk, —N(Alk)₂, —N(alk)(phenylalkyl),—N(Alk)(aminoalkyl) —N(Alk)(alkylaminoalkyl),—N(Alk)(dialkylaminoalkyl); carboxyl in free form or esterified withalkyl, all the phenyl are optionally substituted with alkylenedioxy, allthe alkyl are optionally substituted with one or more radicals chosenfrom piperazinyl, itself optionally substituted with Alk, Alk-OH andpyridyl; imidazolyl; morpholinyl; pyrrolidyl; piperidyl, itselfoptionally substituted with one or two alk; azepanyl optionallysubstituted with oxo, all the pyrrolidyl and quinazolinyl are optionallysubstituted with oxo or thioxo, all the alkyl and alkoxy being linear orbranched and containing not more than 6 carbon atoms, all the cycloalkylcontaining not more than 7 carbon atoms, and n is 0 to 2, or a racemic,enantiomeric or diastereoisomeric isomer form of the compound of formulaI, or an addition salt with a mineral or organic acid or with a mineralor organic base thereof.
 48. The compound according to claim 47 whereinthe radical


49. The compound of formula (IA):

in which: Y1A is —OCF₃, —S(O)—CF₃ or —SO₂CHF₂, B2a is 4-quinolyl or4-pyridyl optionally substituted with one or more radicals chosen fromthe definition of Y2A, Y2A is defined as Y2, R2A and R3A taken togetherwith the carbon atom to which they are attached form a C₃-C₁₀ cycloalkylor heterocyclyl, all the alkyl and phenyl above are optionallysubstituted with one or more radicals chosen from halogen, —OH, alk,—O-alk, —OCF₃, —S(O)—CF₃, —CF₃, —NH₂, —NH-Alk and —N(Alk)₂, and Y2 ishydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl,heterocyclyl, aryl, heteroaryl, —O—alkenyl, —O-alkynyl, —O-cycloalkyl,—S(O)_(n)-alkyl, —S(O)_(n)-alkenyl, —S(O)_(n)-alkynyl,—S(O)_(n)-cycloalkyl, —COOR13, —OCOR13, NR5R6, CONR5R6, —S(O)—NR5R6,—NR10-CO—R13, —NR10-SO₂—R13, NH—SO₂—NR5R6, —NR10-CO—NR5R6,—NR10-CS—NR5R6 or NR10-COOR13, all of which are optionally substituted,R5 and R6, which may be identical or different, are hydrogen, alkyl,alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl orheteroaryl, or R5 and R6 taken together with the nitrogen atom to whichthey are attached form a 3- to 10-membered heterocyclyl containing oneor more hetero atoms chosen from O, S, N and NR7, R7 is hydrogen, alkyl,cycloalkyl, phenyl, acyl, —S(O)₂Alk, —S(O)₂Aryl, —S(O)₂heteroaryl or—S(O)₂NR5R6, except for Y1A, B2a, R2A, and R3A, all the carbocyclyl,heterocyclyl, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl,aryl and heteroaryl above, and also the ring formed by R5 and R6 withthe nitrogen atom to which they are attached, are optionally substitutedwith one or more substituents, which may be identical or different,selected from the group consisting of halogen, cyano, hydroxyl, alkoxy,—CF₃, nitro, aryl, heteroaryl, —C(═O)—OR9, —C(═O)—R8, —NR11R12,—C(═O)—NR11R12, —N(R10)-C(═O)—R8, —N(R10)-C(═O)—OR9,—N(R10)-C(═O)—NR11R12, —N(R10)-S(O)—R8, —S(O)_(n)—R8,—N(R10)-S(O)—NR11R12 and —S(O)—NR11R12, except for B2a, all the aryl andheteroaryl above are optionally substituted with one or moresubstituents selected from the group consisting of alkyl, alkoxy andalkylenedioxy, except for B2a, R2A, and R3A, all the cyclic radicalsabove, and also the ring formed by R5 and R6 with the nitrogen atom towhich they are attached, are optionally substituted with one or moresubstituents selected from the group consisting of oxo and thioxo, R8 isalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl,heterocyclylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, R9 isdefined as R8 or is hydrogen, R10 is hydrogen or alkyl, R11 and R12,which may be identical or different, are hydrogen, C₃-C₆ cycloalkyl,C₁-C₄ alkyl, or phenyl, optionally substituted with one or moresubstituents, which may be identical or different, selected from thegroup consisting of halogen, cyano, hydroxyl, alkoxy, —CF₃, nitro,phenyl, and free, salified, esterified or amidated carboxyl, or R11 andR12 taken together with the nitrogen atom to which they are attachedform a 5- to 7-membered cyclic radical containing one or more heteroatoms chosen from O, S, N and NR7, R13, which may be identical to ordifferent from R5 or R6, is defined as R5 or R6, and n is 0 to 2, or aracemic, enantiomeric or diastereoisomeric isomer form of said compound,or an addition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 50. The compound according to claim 49 whereinY1A, B2a, R2A and R3A are as defined in claims 49 and Y2A is halogen,—OH, -alk, —Oalk, —Oacyl, —NR5AR6A, —CO2H, —CO2alk, —CO——NR5AR6A,—S(O)—CF₃, —NH—S(O)—CF₃ or phenyl, alk is a linear or branched alkylradical containing not more than 6 carbon atoms, all the alkyl, alkoxyand phenyl are optionally substituted; R5A and R6A, which may beidentical or different, are hydrogen, alkyl, cycloalkyl or phenyl, thealkyl and phenyl are optionally substituted, or R5A and R6A takentogether with the nitrogen atom to which they are attached form cyclicradical chosen from pyrrolidyl, piperidyl, piperazinyl, morpholinyl,indolinyl, tetrahydroquinolyl and azetidinyl, all the alkyl, alkoxy andphenyl are optionally substituted with one or more radicals chosen fromhalogen, —OH, alk, —Oalk, —OCF₃, —S(O)—CF₃, —CF₃, —NH₂, —NH-Alk and—N(Alk)₂, and n is 0 to 2, or a racemic, enantiomeric ordiastereoisomeric isomer form of said compound, or an addition salt witha mineral or organic acid or with a mineral or organic base thereof. 51.The compound according to claim 49 wherein Y1A is OCF₃, SCF₃ orS(O)2-CF₃, B2a is a 4-quinolyl or 4-pyridyl radical optionallysubstituted with one or two radicals chosen from halogen, —OH, alk,—Oalk, —CO2H, -CO2alk, —NR5AR6A, —CF₃, —OCF₃ and optionally substitutedphenyl, R5A and R6A, which may be identical or different, are hydrogen,alkyl, cycloalkyl or phenyl, the alkyl and phenyl radicals beingoptionally substituted, or R5A and R6A taken together with the nitrogenatom to which they are attached form a cyclic radical chosen frompyrrolidyl, piperidyl, piperazinyl, morpholinyl, piperazinyl andazetidinyl radicals, R2A and R3A taken together with the carbon atom towhich they are attached form a C₃-C₆ cycloalkyl or heterocyclyl radical,all the alkyl and phenyl radicals being optionally substituted with oneor more radicals chosen from halogen, OH, alk, Oalk, OCF₃, S(O)—CF₃,—CF₃, NH₂, NHalk and N(Alk)₂, or a racemic, enantiomeric ordiastereoisomeric isomer form of said compound, or an addition salt witha mineral or organic acid or with a mineral or organic base thereof. 52.The compound according to claim 49 wherein Y1A is OCF₃, —SCF₃ or—S(O)₂—CF₃, B2a is 4-quinolyl or 4-pyridyl optionally substituted withone or two radicals chosen from halogen, —OH, alk and —Oalk, and R2A andR3A taken together with the carbon atom to which they are attached forma C₃-C₆ cycloalkyl, or a racemic, enantiomeric or diastereoisomericisomer form of said compound, or an addition salt with a mineral ororganic acid or with a mineral or organic base thereof.
 53. The compoundaccording to claim 49 wherein Y la is —OCF₃, —SCF₃ or —S(O)₂CF₃, and R2Aand R3A taken together with the carbon atom to which they are attachedform cyclopropyl, or a diastereoisomeric isomer form of said compound,or an addition salt with a mineral or organic acid or with a mineral ororganic base thereof.
 54. A compound selected from the group consistingof:4-quinol-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-quinol-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-pyrid-4-ylmethyl-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-pyrid-4-ylmethyl-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-quinol-4-ylmethyl-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-(3-methylpyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethoxyphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethylsulfanylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;and4-(3-hydroxypyrid-4-ylmethyl)-6-(4-trifluoromethanesulfonylphenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;or a racemic, enantiomeric or diastereoisomeric isomer form of thecompound of formula I, or an addition salt with a mineral or organicacid or with a mineral or organic base thereof.
 55. A pharmaceuticalcomposition comprising a pharmaceutically effective amount of a compoundaccording to claim 1 and a pharmaceutically acceptable adjuvant.
 56. Amethod for treating a patient suffering from rheumatoid arthritis,comprising administering to the patient a physiologically effectiveamount of the compound according to claim 1.